5-HT Receptor · 2020. 7. 9. · 5-HT Receptor Antagonists, Agonists, Inhibitors & Modulators...

5-HT ReceptorSerotonin Receptor 5-hydroxytryptamine Receptor

5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs)found in the central and peripheral nervous systems Type 5-HT1 5-HT2 5-HT3 5-HT4 5-HT5 5-HT6 5-HT7 They mediate bothexcitatory and inhibitory neurotransmission The serotonin receptors are activated by the neurotransmitter serotonin which acts astheir natural ligand The serotonin receptors modulate the release of many neurotransmitters as well as many hormones Theserotonin receptors influence various biological and neurological processes such as aggression anxiety appetite cognitionlearning memory mood nausea sleep andthermoregulation The serotonin receptors are the target of a variety of pharmaceuticaldrugs including many antidepressants antipsychotics anorecticsantiemetics gastroprokinetic agents antimigraine agentshallucinogens and entactogens

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5-HT Receptor Antagonists Agonists Inhibitors Modulators amp Activators

(4E)-SUN9221Cat No HY-U00367

(4E)-SUN9221 is a potent antagonist of and withα1-adrenergic receptor 5-HT2 receptor

antihypertensive and anti-platelet aggregationactivities

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

(R)-Mirtazapine ((R)-Org3770 (R)-6-Azamianserin) Cat No HY-B0352B

(R)-Mirtazapine ((R)-Org3770) is a R(minus)-enantiomerof Mirtazapine with antinociceptive properties inan animal model of acute thermal nociception(R)-Mirtazapine is a antagonist5-HT receptor3

(R)-Mirtazapine is mainly metabolized by CYP3A4


(R)-Mirtazapine D3 ((R)-Org3770 D3 (R)-6-Azamianserin D3) Cat No HY-B0352BS

(R)-Mirtazapine D3 ((R)-Org3770 D3) is a deuteriumlabeled (R)-Mirtazapine (R)-Mirtazapine is aR(minus)-enantiomer of Mirtazapine withantinociceptive properties in an animal model ofacute thermal nociception (R)-Mirtazapine is a

antagonist5-HT receptor3


(R)-Praziquantel D11Cat No HY-126057S

(R)-Praziquantel D11 is the deuterium labeled(R)-Praziquantel (R)-Praziquantel the activeenantiomer of Praziquantel is a partial agonistof the human 5-HT2B receptor (R)-Praziquantelacts as an antischistosomal eutomer


(RR)-Palonosetron HydrochlorideCat No HY-A0021C

(RR)-Palonosetron Hydrochloride is the activeenantiomer of Palonosetron

Purity 9961Clinical Data No Development ReportedSize 1 mg 5 mg

(Rac)-Rotigotine hydrochlorideCat No HY-15394

(Rac)-Rotigotine hydrochloride is a racemate ofRotigotine

Purity 9776Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg

(Rac)-WAY-161503Cat No HY-103138A

(Rac)-WAY-161503 is a potent selective highlyaffinity agonist with a of 45-HT receptor2C Ki

nM and an EC of 12 nM (Rac)-WAY-16150350

displays higher affinity for 5-HT than 5-HT2C 2A

and 5-HT receptors (Rac)-WAY-161503 has2B

anti-obesity and antidepressant effects

Purity gt990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg

(S)-Mirtazapine ((S)-Org3770 (S)-6-Azamianserin) Cat No HY-B0352A

(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomerof Mirtazapine with pronociceptive properties inan animal model of acute thermal nociception(S)-Mirtazapine is a stereoselective 5-HT2

antagonist (S)-Mirtazapine isreceptormetabolized by CYP2D6 and CYP1A2


(S)-Mirtazapine D3 ((S)-Org3770 D3 (S)-6-Azamianserin D3) Cat No HY-B0352AS

(S)-Mirtazapine D3 ((S)-Org3770 D3) is a deuteriumlabeled (S)-Mirtazapine (S)-Mirtazapine is aS(+)-enantiomer of Mirtazapine with pronociceptiveproperties in an animal model of acute thermalnociception(S)-Mirtazapine is a stereoselective



(Z)-ThiothixeneCat No HY-108324

(Z)-Thiothixene is an antagonist of serotonergic extracted from patent US 20150141345 A1receptor

Purity 9976Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg

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(plusmn)-Fabesetron hydrochloride ((plusmn)-FK1052) Cat No HY-101638

(plusmn)-Fabesetron hydrochloride ((plusmn)-FK1052) is theracemate of Fabesetron hydrochloride which is apotent and receptor dual antagonist5-HT3 5-HT4


2-O-MethylisoliquiritigeninCat No HY-N1745

2-O-Methylisoliquiritigenin isolated from the species up-regulates andArachis 5-HT NE DA

pathways but does not put a veryGABAsignificant effect on ne NE pathway


2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine

2-Methylserotonin 2-Me-5-HT) Cat No HY-19358

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is apotent and selective agonist5-HT receptor3

2-Methyl-5-HT is shown to displayanti-depressive-like effects

Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine

hydrochloride 2-Methylserotonin hydrochloride hellip) Cat No HY-19358A

2-Methyl-5-HT hydrochloride(2-Methyl-5-hydroxytryptamine hydrochloride) is apotent and selective agonist5-HT receptor3

2-Methyl-5-HT hydrochloride is shown to displayanti-depressive-like effects


2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate

2-Methylserotonin maleate 2-Me-HT maleate) Cat No HY-19358B

2-Methyl-5-HT maleate(2-Methyl-5-hydroxytryptamine maleate) is a potentand selective agonist5-HT receptor3

2-Methyl-5-HT maleate is shown to displayanti-depressive-like effects


3-Hydroxy agomelatineCat No HY-133111

3-Hydroxy agomelatine is a metabolite ofAgomelatine 3-Hydroxy agomelatine is a 5-HT2C

antagonist with an of 32 μM and areceptor IC50

of 18 μMKi

Purity gt98Clinical Data No Development ReportedSize 5 mg

5-Carboxamidotryptamine maleate (5-CT maleate) Cat No HY-100942

5-Carboxamidotryptamine maleate (5-CT maleate) isa potent and5-HT1A 5-HT1B 5-HT1D 5-HT5

agonist5-HT receptors7


5-HT1A modulator 1Cat No HY-100290

5-HT1A modulator 1 displays very high affinitiesfor the and 5HT1A adrenergic α1 dopamine

with s of 2 plusmn03 nM 10 plusmn 3 nMD receptor2 IC50

and 40 plusmn9 nM respectively


5-HT1A modulator 2 hydrochlorideCat No HY-136621

5-HT1A modulator 2 hydrochloride a derivative of8-OH-DPAT (HY-112061) is a modulator of 5-HT1A

with a of 53 nM for 5-HT bindingKi 1A

Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg

5-HT2 antagonist 1Cat No HY-U00365

5-HT2 antagonist 1 is a potent antagonist of with weak 5-HT2 receptor α1 adrenoceptor

blocking activity



5-HT2A antagonist 1Cat No HY-U00286

5-HT2A antagonist 1 is a antagonist5-HT2Aextracted from patent US5728835A and JP 10077275-HT2A antagonist 1 may be useful in treatment ofgastrointestinal disorders circulatory disorders



5-HT3 antagonist 1 is a potent and selectiveantagonist of serotonin 3 (5-HT3) receptor



5-HT3 antagonist 2 is a receptor5-HT3antagonist



5-HT3 antagonist 3 (Compound 15b) is ahigh-affinity antagonist 5-HT35-HT3 receptorantagonist 3 binds to 5-HT3 receptors in rat braincortical membranes with of 025 nMKi


5-HT3-In-1Cat No HY-U00413

5-HT3-In-1 is extracted from patent EP0748807A1compound example 8 It shows inhibition5-HT3activity


5-HT67 antagonist 1Cat No HY-101622

5-HT67 antagonist 1 is a multifunctional ligandthat antagonizes and receptors5-HT672A D2without interacting with M1 receptors and hERGchannels


5-HT7 agonist 1Cat No HY-109527

5-HT7 agonist 1 is a selective 5-HT7 receptoragonist with an of 22293 nM can be usedIC50

for the 5-HT7 receptor related disease such asCNS disorders


7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine) Cat No HY-133112

7-Desmethyl-3-hydroxyagomelatine(3-Hydroxy-7-desmethyl agomelatine) a metaboliteof Agomelatine has less activity thanAgomelatine Agomelatine is a melatonergic( and ) agonist and MT1 MT2 serotonergic( ) antagonist5HT2C


7-Desmethyl-agomelatineCat No HY-133113

7-Desmethyl-agomelatine is a metabolite ofAgomelatine Agomelatineis a potent agonist atmelatonin receptors (MT1 and MT2) and also is anantagonist of 5-HT2C


8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) Cat No HY-15688

8-Hydroxy-DPAT hydrobromide (8-OH-DPAThydrobromide) is a potent and selective 5-HT1A

agonist with a of 819 8-Hydroxy-DPATpIC50

hydrobromide has selectivity of almost 1000 foldfor a subtype of the 5-HT binding site1



8-OH-DPAT (8-Hydroxy-DPAT) Cat No HY-112061

8-OH-DPAT is a potent and selective agonist5-HTwith a of 819 for 5-HT1A and a of 466 nMpIC50 Ki

for 5-HT7 8-OH-DPAT weakly binds to 5-HT1B (pIC 50

542) 5-HT (pIC lt5)50

Purity gt980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg

AbaperidoneCat No HY-101619

Abaperidone is a potent antagonist of and 5-HT receptor2A dopamine D receptor2

with s of 62 and 17 nMIC50


Adoprazine (SLV313) Cat No HY-14782

Adoprazine a potential atypical antipsychoticbearing potent D2 receptor antagonist and 5-HT1Areceptor agonist properties

Purity 9810Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg

Agomelatine (S-20098) Cat No HY-17038

Agomelatine (S-20098) is a specific agonist of and receptors with s of 01 006MT1 MT2 Ki

012 and 027 nM for CHO-hMT1 HEK-hMT1CHO-hMT2 and HEK-hMT2 respectively

Purity 9877Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Agomelatine (L(+)-Tartaric acid) (S-20098 L(+)-Tartaric acid) Cat No HY-17038B

Agomelatine L(+)-Tartaric acid (S-20098L(+)-Tartaric acid) is a specific agonist of

and receptors with s of 01 006MT1 MT2 Ki



Agomelatine hydrochloride (S-20098 hydrochloride) Cat No HY-17038A

Agomelatine hydrochloride (S-20098 hydrochloride)is a specific agonist of and MT1 MT2receptors with s of 01 006 012 and 027 nMKi

for CHO-hMT1 HEK-hMT1 CHO-hMT2 and HEK-hMT2respectively


AlmotriptanCat No HY-B0383A

Almotriptan is a 5-HT1B1D-receptor agonist usedto treat migraine

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Almotriptan malate (PNU180638) Cat No HY-B0383

Almotriptan Malate is a 5-HT1B1D-receptor agonistused to treat migraine

Purity 9949Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Alniditan (Alnitidan) Cat No HY-101698

Alniditan is a potent 5-HT receptors1B1D

agonist with of 17 and 13 nM in HEK293IC50

cells and value of 896 and 940 forpKi

5-HT receptors respectively1B1D


Alosetron (GR 68755 GR 68755X) Cat No HY-70050A

Alosetron (GR 68755) is a potent and highlyselective serotonin antagonist5-HT3 receptorAlosetron is used for the research of irritablebowel syndrome (IBS)

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg


Alosetron ((Z)-2-butenedioate) (GR 68755

((Z)-2-butenedioate) GR 68755X ((Z)-2-butenedioate)) Cat No HY-70050B

Alosetron (GR 68755) (Z)-2-butenedioate is apotent and highly selective serotonin 5-HT3

antagonist Alosetron (Z)-2-butenedioatereceptoris used for the research of irritable bowelsyndrome (IBS)


Alosetron (Hydrochloride(1X)) (GR 68755

(Hydrochloride(1X)) GR 68755X (Hydrochloride(1X))) Cat No HY-70050

Alosetron (GR 68755) Hydrochloride(1X) is apotent and highly selective serotonin 5-HT3

antagonist Alosetron Hydrochloride(1X)receptoris used for the research of irritable bowelsyndrome (IBS)


Alosetron Hydrochloride (GR 68755C GR 68755 Hydrochloride

GR 68755X Hydrochloride) Cat No HY-70050C

Alosetron Hydrochloride (GR 68755C) is a potentand highly selective serotonin 5-HT3 receptorantagonist Alosetron Hydrochloride is used forthe research of irritable bowel syndrome (IBS)


Alprenolol ((RS)-Alprenolol dl-Alprenolol) Cat No HY-B1517

Alprenolol is a non-selective beta blocker as wellas 5-HT1A receptor antagonist The reference foradministration is 10 mgkg

Purity 9987Clinical Data LaunchedSize 50 mg 100 mg

Alprenolol hydrochloride ((RS)-Alprenolol hydrochloride

dl-Alprenolol hydrochloride) Cat No HY-B1517A

Alprenolol (hydrochloride) is a non-selective betablocker as well as 5-HT1A receptor antagonist Thereference for administration is 10 mgkg


Alverine citrate (NSC 35459) Cat No HY-B0500

Alverine citrate is a receptor5-HT1A

antagonist with an of 101 nMIC50

Purity 9943Clinical Data LaunchedSize 10 mM times 1 mL 500 mg 1 g 5 g 10 g

Amitriptyline hydrochlorideCat No HY-B0527A

Amitriptyline hydrochloride is an inhibitor of andserotonin reuptake transporter (SERT)

with snoradrenaline reuptake transporter (NET) Ki

of 345 nM and 133 nM for human SERT and NETrespectively

Purity 9956Clinical Data LaunchedSize 10 mM times 1 mL 500 mg 1 g 5 g

Ansofaxine hydrochloride (LY03005 LPM570065) Cat No HY-U00096

Ansofaxine hydrochloride (LY03005 LPM570065) is atriple reuptake inhibitor inhibits serotonin

and reuptake with dopamine norepinephrine IC50

values of 723 491 and 763 nM respectively

Purity 9985Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 20 mg 50 mg 100 mg

AP521Cat No HY-100166

AP521 is an agonist of human 5-HT receptor1A

with an of 94 nMIC50


AR-A 2 (AR-A 000002) Cat No HY-107018

AR-A 2 is a selective 5-HT receptor1B

antagonist with high affinity to guinea pigcortex and recombinant guinea pig5HT1B1D

( =024 and 047 nM) and with5-HT receptors1B Ki

10-fold lower affinity to guinea pig 5-HT1D

( 5 nM) and shows an ofhellipreceptor Ki EC50



Aripiprazole (OPC-14597) Cat No HY-14546

Aripiprazole (OPC-14597) is a human 5-HT1Areceptor partial agonist with a Ki of 42 nM

Purity 9998Clinical Data LaunchedSize 100 mg 200 mg 500 mg 1 g

ArotinololCat No HY-122537A

Arotinolol is a nonselective αβ-adrenergic blocker and a vasodilating β-blockerreceptor

Arotinolol also shows potency for inhibiting thebinding of the radioligand I-ICYP to125

-serotonergic receptor sites5HT1B


AS19Cat No HY-103142

AS19 is a potent selective 5-HT receptor7

agonist with an value of 083 nM and a ofIC50 Ki

06 nM AS19 is selective for over5-HT7

5-HT 5-HT 5-HT and 5-HT receptors1A 1B 1D 5A

( s = 897 nM 490 nM 66 nM and 985 nMKi

respectively)


Asenapine (Org 5222) Cat No HY-10121

Asenapine is an antagonist of serotonin receptors(5-HT 5-HT 5-HT 5-HT 5-HT )2A 2B 2C 6 7

(α α α α )adrenoceptors 1 2A 2B 2C

(D D D ) anddopamine receptors 2 3 4

(H H ) with shistamine receptors 1 2 pKi

of 84-105 89-95 89-94 andhellip


Asenapine hydrochlorideCat No HY-16567

Asenapine hydrochloride an antipsychotic is a (1A 1B 2A 2B 2C 5A 6 7) and 5-HT

receptor antagonist withDopamine (D D D )2 3 4

values of 003-40 nM for 5-HT and 13 042Ki

11 nM for Dopamine receptor respectively


Asenapine maleate (Org 5222 maleate) Cat No HY-11100

Asenapine maleate is a (1A 1B 2A 2B 2C5-HT5A 6 7) and antagonist with values ofD2 Ki

003-40 nM 13nM respectively and anantipsychotic

Purity 9995Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg 500 mg

AsimilobineCat No HY-N7512

Asimilobine is an aporphine isoquinoline alkaloidisolated from plant species of Magnolia obobataThun Asimilobine is a biosynthesisdopamineinhibitor and a antagonistserotonergic receptorAsimilobine shows an andantimalarialanti-cancer activity


AVN-492Cat No HY-101924

AVN-492 is a very specific and highly-selectiveantagonist with picomolar affinity to 5-HT6R( =91 pM)Ki


Azasetron hydrochloride (Y-25130 hydrochloride) Cat No HY-B0068

Azasetron (Y-25130) hydrochloride a benzamidederivative is a potent and selective 5-HT3receptor antagonist Azasetron is used in thestudy for Chemotherapy-induced nausea and vomiting(CINV)


Befiradol (NLX-112 F13640) Cat No HY-14785

Befiradol (NLX-112) is a selective 5-HT1Areceptor agonist



Befiradol hydrochloride (NLX-112 hydrochloride F 13640 hydrochloride) Cat No HY-14785A

Befiradol hydrochloride (NLX-112 hydrochloride) isa selective receptor agonist5-HT1A

Purity 9922Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bemesetron (MDL 72222) Cat No HY-B1541

Bemesetron (MDL 72222) is a selective 5-HT3

antagonist with an of 033 nMreceptor IC50

Neuroprotective effect


BGC20-761Cat No HY-21995

BGC20-761 is a selecvtive and 5-HT6 dopamine antagonist (human receptor valuesreceptor Ki

5-HT6 (20 nM) 5-HT2A (69 nM) D2 (140 nM)BGC20-761 can enhance long-term memory BGC20-761has potential utility as an antipsychotic agent


Blonanserin (AD-5423) Cat No HY-13575

Blonanserin (AD-5423) is a potent and orallyactive ( =0812 nM)5-HT2A Ki

and (dopamine D2enspreceptor Ki

=0142 nM) antagonist


Blonanserin D5 (AD-5423 D5) Cat No HY-13575S1

Blonanserin D5 (AD-5423 D5) is a deuterium labeledBlonanserin Blonanserin is a dopamine

antagonist and an atypicalD 5-HT receptor2 2

antipsychotic


Blonanserin D8 (AD-5423 D8) Cat No HY-13575S



antipsychotic


Brexpiprazole (OPC-34712) Cat No HY-15780

Brexpiprazole (OPC-34712) an atypicalantipsychotic drug is a partial agonist of human

and with s of 0125-HT1A dopamine receptor Ki

nM and 03 nM respectively Brexpiprazole is alsoa receptor antagonist with a of 0475-HT2A Ki

nM


Brexpiprazole S-oxide (DM-3411) Cat No HY-133152

Brexpiprazole S-oxide (DM-3411) is a mainmetabolite of Brexpiprazole and is metabolized bycytochrome P450 3A4 (CYP3A4)


Brexpiprazole S-oxide D8 (DM-3411 D8) Cat No HY-133152S

Brexpiprazole S-oxide D8 (DM-3411 D8) is adeuterium labeled Brexpiprazole S-oxideBrexpiprazole S-oxide is a main metabolite ofBrexpiprazole and is metabolized by cytochromeP450 3A4 (CYP3A4)


Brilaroxazine (RP5063) Cat No HY-109112

Brilaroxazine (RP5603) is a potent and orallyactive multimodal dopamine (DA)serotonin

modulator(5-HT)



BRL 54443Cat No HY-13221

BRL 54443 is a potent receptor agonist5-HT1E1F

( values are 11 nM and 07 nM respectively)Ki

displays gt 30-fold selectivity over other 5-HTand dopamine receptors

Purity 9939Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg

BRL-15572 dihydrochlorideCat No HY-13200

BRL-15572 dihydrochloride is a selectiveantagonist of displays high affinity forh5-HT1D

BRL-15572 dihydrochlorideh5-HT1D receptorscould be useful pharmacological agents tocharacterise mediated responses5-HT1D receptor


Bromperidol (R-11333) Cat No HY-B0901

Bromperidol is a butyrophenone derivative is apotent and long-acting neuroleptic used as anantipsychotic in the treatment of schizophrenia

Purity 9802Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg

Buspirone hydrochlorideCat No HY-B1115

Buspirone hydrochloride is an anxiolyticpsychotropic drug is used to treat generalizedanxiety disorder (GAD)

Purity 9992Clinical Data LaunchedSize 10 mM times 1 mL 100 mg

Cariprazine (RGH-188) Cat No HY-14763

Cariprazine is a novel antipsychotic drugcandidate that exhibits high affinity for the D3

( =0085 nM) and ( =049 nM) receptors andKi D2 Ki

moderate affinity for the receptor5-HT1A

( =26 nM)Ki

Purity 9935Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Cariprazine hydrochloride (RGH188 hydrochloride) Cat No HY-14763A

Cariprazine hydrochloride is a novel antipsychoticdrug candidate that exhibits high affinity for the

( =0085 nM) and ( =049 nM)D3 Ki D2 Ki

receptors and moderate affinity for the 5-HT1A

receptor ( =26 nM)Ki


CART(62-76)(humanrat)Cat No HY-P1303

CART(62-76)(humanrat) is a neuropeptide (62-76residues of the CART peptide) withneurotransmitter-like effects


CART(62-76)(humanrat) TFACat No HY-P1303A

CART(62-76)(humanrat) TFA is a neuropeptide(62-76 residues of the CART peptide) withneurotransmitter-like effects


Chlorpromazine D6 hydrochlorideCat No HY-B0407AS

Chlorpromazine D6 hydrochloride is the deuteriumlabeled Chlorpromazine Chlorpromazine is aninhibitor of dopamine receptor 5-HT receptorpotassium channel sodium channel

Purity gt990Clinical Data LaunchedSize 10 mM times 1 mL 1 mg 5 mg 10 mg

Chlorpromazine hydrochlorideCat No HY-B0407A

Chlorpromazine hydrochloride is an antagonist ofthe dopamine D2 5HT2A potassium channeland Chlorpromazine binds with D2sodium channeland 5HT2A with s of 363 nM and 83 nMKi

respectively

Purity 9990Clinical Data LaunchedSize 500 mg 1 g 5 g


Cinanserin hydrochloride (SQ 10643) Cat No HY-100943

Cinanserin hydrochloride (SQ 10643) is a potentselective and highly affinity 5-HT receptor2

antagonist with a of 41 nM CinanserinKi

hydrochloride has a much higher binding affinityfor the than for the 5-HT receptor (5-HT2 1 Ki

of 3500 nM)


cis-(Z)-Flupentixol dihydrochloride (cis-(Z)-Flupenthixol dihydrochloride) Cat No HY-15856

cis-(Z)-Flupentixol dihydrochloride is a potentand selective antagonist withDA D1D2 receptor

values of 038 nM and 7 nM for D2 receptor andKi

respectively5-HT2A


cis-Urocanic acid ((Z)-Urocanic acid cis-UCA) Cat No HY-113008A

cis-Urocanic acid is a agonist5-HT2A receptorcis-Urocanic acid binds to with5-HT receptorrelatively high affinity ( =46 nM)Kd

cis-Urocanic acid is an immune modulator thatinduces immunosuppression by binding to the 5-HT2Areceptor

Purity 9992Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg

Cisapride (R 51619 (plusmn)-Cisaprid) Cat No HY-14149

Cisapride(R 51619) is a nonselective 5-HT4receptor agonist it is also a potent hERGpotassium channel inhibitor


Clocapramine (Clocarpramine 3-Chlorocarpipramine) Cat No HY-B2073

Clocapramine is an antagonist of the D2

5-HT receptors2A


Clocapramine hydrochloride hydrate (3-Chlorocarpipramine hydrochloride hydrate) Cat No HY-B2073A

Clocapramine hydrochloride hydrate is anantagonist of the and D2 5-HT receptors2A


CP-809101 hydrochlorideCat No HY-15543A

CP-809101 hydrochloride is a potent and selective5-HT2C receptor agonist with pEC50 of996719681 for human 5-HT2C5-HT2B5-HT2Areceptors respectively


CyamemazineCat No HY-14264

Cyamemazine is a neuroleptic agent that containsthe phenothiazine chromophore Cyamemazine isoften used as an anxiolytic Cyamemazine is apotent ( of 12 nM) ( = 155-HT3 Ki 5-HT2A Ki

nM) and ( of 75 nM) receptors5-HT2C Ki

antagonist with antipsychotic activity


Cyclobenzaprine hydrochloride (MK130 hydrochloride) Cat No HY-B0740

Cyclobenzaprine hydrochloride (MK130hydrochloride) is a skeletal muscle relaxant and acentral nervous system (CNS) depressant Target5-HT Receptor 2A Cyclobenzaprine hydrochloride isa skeletal muscle relaxant and a central nervoussystem (CNS) depressant


Cyproheptadine hydrochlorideCat No HY-B0366A

Cyproheptadine hydrochloride is a 5-HT2A

antagonist with antidepressant andreceptorantiserotonergic effects Cyproheptadinehydrochloride has antiplatelet andthromboprotective activities

Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg 1 g


Cyproheptadine hydrochloride sesquihydrateCat No HY-B1165

Cyproheptadine hydrochloride sesquihydrate is anantihistamine and is an antagonist of serotoninand histamine2


Dehydroaripiprazole (OPC-14857 DM-14857) Cat No HY-100665

Dehydroaripiprazole (OPC-14857) is an activemetabolite of Aripiprazole Aripiprazole is anantipsychotic agent and is metabolized by CYP3A4and CYP2D6 forming mainly DehydroaripiprazoleDehydroaripiprazole has with antipsychoticactivity equivalent to Aripiprazole

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Deramciclane (EGIS-3886) Cat No HY-101630

Deramciclane has a high affinity for and5-HT2A

receptors it acts as an antagonist at5-HT2C

both receptor subtypes and has inverse agonistproperties at the 5-HT receptors without direct2C

stimulatory agonist


Dihydroergotamine mesylateCat No HY-B0670A

Dihydroergotamine mesylate is an ergot alkaloidused to treat migraines


Dolasetron (MDL-73147) Cat No HY-B0750

Dolasetron(MDL-73147) is a serotonin 5-HT3receptor antagonist used to treat nausea andvomiting following chemotherapy

Purity gt980Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg

Dolasetron Mesylate (MDL-73147EF) Cat No HY-B0750A

Dolasetron Mesylate (MDL-73147EF) is a serotonin5-HT3 receptor antagonist used to treat nausea andvomiting following chemotherapy


Dolasetron Mesylate hydrate (MDL-73147EF hydrate) Cat No HY-B0750B

Dolasetron Mesylate hydrate (MDL-73147EF hydrate)is a serotonin 5-HT3 receptor antagonist used totreat nausea and vomiting following chemotherapy


DonitriptanCat No HY-106157

Donitriptan is a potent high efficacy agonist ats with s of 94 and 935-HT receptor1B1D pKi

respectively


Eletriptan hydrobromide (Eletriptan HBr) Cat No HY-A0010

Eletriptan HBr is a selective 5-HT1B and 5-HT1Dreceptor agonist with Ki of 092 nM and 314 nMrespectively


Eltoprazine (DU 28853) Cat No HY-16687

Eltoprazine(DU28853) is a serenic orantiaggressive agent which as an agonist at the5-HT1A and 5-HT1B receptors and as an antagonistat the 5-HT2C receptor

Purity gt950Clinical Data Phase 2Size 1 mg 5 mg


Eltoprazine hydrochloride (DU 28853 hydrochloride) Cat No HY-16687A

Eltoprazine hydrochloride (DU 28853 hydrochloride)is a serenic or antiaggressive agent which as anagonist at the 5-HT1A and 5-HT1B receptors and asan antagonist at the 5-HT2C receptor


EMD 56551Cat No HY-19134

EMD 56551 is a potent and selective 5-HT1A agonist EMD 56551 exerts anxiolyticreceptor

activity


Eplivanserin (SR-46349) Cat No HY-10792

Eplivanserin is a potent selective and orallyavailable antagonist with an5-HT receptor2

of 58 nM in rat cortical membrane and aIC50

of 114 nMKd


Eplivanserin (mixture) (SR-46349 (mixture)) Cat No HY-10792A

Eplivanserin mixture (SR-46349 mixture) is aselective inhibitor and aserotonin reuptake

antagonist extracted from5-HT receptor2A

patent WO 2005002578 A1

Purity 9995Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Eptapirone (F 11440) Cat No HY-19946

Eptapirone (F11440) is a potent selective highefficacy 5-HT1A receptor agonist with markedanxiolytic and antidepressant potential


F-15599 (NLX-101) Cat No HY-19863

F-15599 is a highly selective G-protein biased agonist with of 34 nM5-HT1A receptor Ki


Fabesetron (FK1052 free base) Cat No HY-105201

Fabesetron (FK1052) is an orally active 5-HT3

antagonist with receptor 5-HT receptor4

antagonistic activity Fabesetron (FK1052) can beused in the study for both acute and delayedemesis induced by cancer chemotherapy


Facinicline hydrochloride (RG3487 hydrochloride) Cat No HY-108057A

Facinicline hydrochloride (RG3487 hydrochloride)is an orally active partialnicotinic α7 receptoragonist with a of 6 nM for α7 human nAChRKi

Facinicline hydrochloride (RG3487 hydrochloride)improves cognition and sensorimotor gating inrodents

Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

Fananserin (RP 62203) Cat No HY-103104

Fananserin (RP 62203) is an orally bioavailablepotent and selective 5-hydroxytryptamine2

receptor antagonist with a of 037(5-HT )2 Ki

nM for the rat 5-HT receptor2A


FlesinoxanCat No HY-121653

Flesinoxan is a hypotensive agent and a potenthigh affinity and selective5-hydroxytryptamine1A (5-HT1A) receptoragonist with an value of 24 nM FlesinoxanEC50

also has effective anxiolyticantidepressanteffects

Purity 9907Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 1 g


Flibanserin (BIMT-17 BIMT-17BS) Cat No HY-A0095

Flibanserin (BIMT-17) is a full agonist of theserotonin ( =1 nM) and an5-HT1A receptor Ki

antagonist of (49 nM)5-HT2A


Flibanserin D4 (BIMT-17 D4 BIMT-17BS D4) Cat No HY-A0095S

Flibanserin D4 is a deuterium labeled Flibanserin(BIMT-17) Flibanserin is a full agonist of theserotonin 5-HT1A receptor (K =1 nM) and ani

antagonist of 5-HT2A (49 nM)


FlopropioneCat No HY-100562

Flopropione is a antagonist and5-HT receptoralso a catechol-o-methyltransferase (COMT)inhibitor Flopropione also as an antispasmodicagent


FlumexadolCat No HY-133024

Flumexadol is an orally active non-narcoticanalgesic Flumexadol is a selective and affinity

agonist with a of 25 nM for5-HT receptor2C Ki

the (+)-enantiomer of Flumexadol and is 40-foldselective over the 5-HT receptor2A


Frovatriptan succinate ((R)-Frovatriptan succinate SB 209509

succinate VML 251 succinate) Cat No HY-B1658B

Frovatriptan succinate ((R)-Frovatriptansuccinate) is a potent high affinity selectiveand orally active ( of 82) and5-HT1B pK50

agonist5-HT receptor1D


Frovatriptan succinate hydrate ((R)-Frovatriptan succinate

hydrate SB 209509 succinate hydrate hellip) Cat No HY-B1658A

Frovatriptan succinate hydrate ((R)-Frovatriptansuccinate hydrate) is a potent high affinityselective and orally active ( of5-HT1B pK50

82) and agonist5-HT receptor1D

Purity gt990Clinical Data LaunchedSize 1 mg

Gamma-Mangostin (γ-Mangostin) Cat No HY-N1957

Gamma-Mangostin is a novel competitive5-hydroxytryptamine 2A (5-HT2A) receptorsantagonist purified from the fruit hull of themedicinal plant Garcinia mangostana

Purity 9990Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg

Geissoschizine methyl etherCat No HY-N2411

Geissoschizine methyl ether a major indolealkaloid found in hook is a major activeUncariacomponent of Yokukansan with psychotropic effectsGeissoschizine methyl ether is potent 5-HT1A

agonistreceptor


GR 113808Cat No HY-103152

GR 113808 is a potent and highly selective antagonist ( = 88) GR5-HT receptor4 pKb

113808 shows 300-fold selectivity over 5-HT 1A

5-HT 5-HT 5-HT and 5-HT receptors1B 2A 2C 3


GR 125743Cat No HY-121392

GR 125743 is a selective receptor5-HT1B1D

antagonist with pK s of 885 and 831 fori

wild-type h5-HT and wild-type h5-HT 1B 1D

respectively GR 125743 is used for the researchof Parkinsons disease and cardiovasculardiseases



Granisetron (BRL 43694) Cat No HY-B0071

Granisetron (BRL 43694) is a serotonin 5-HT3receptor antagonist used as an antiemetic to treatnausea and vomiting following chemotherapy


Granisetron Hydrochloride (BRL 43694A) Cat No HY-B0071A

Granisetron (Hydrochloride) (BRL 43694A) is aserotonin 5-HT3 receptor antagonist used as anantiemetic to treat nausea and vomiting followingchemotherapy


GSK163090Cat No HY-14348

GSK163090 is a potent selective and orally active antagonist with 5-HT receptor1A1B1D pKi

values of 948597 respectively GSK163090inhibits the functional activity of serotoninreuptake transporter (SerT) with a value ofpKi

61

Purity 9995Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

GTS-21 dihydrochloride (DMXB-A DMBX-anabaseine) Cat No HY-14564A

GTS-21 dihydrochloride is a selective alpha7nicotinic acetylcholine receptor (α7-nAChR)agonist with antiinflammatory andcognitionenhancing activities


Harmine (Telepathine) Cat No HY-N0737A

Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitorDYRKwith anticancer and anti-inflammatory activitiesHarmine has a high affinity of 5-HT serotonin2A

with an of 397 nMreceptor Ki

Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg 1 g

Harmine hydrochloride (Telepathine hydrochloride) Cat No HY-N0737

Harmine Hydrochloride (Telepathine Hydrochloride)is a natural inhibitor with anticancer andDYRKanti-inflammatory activities Harmine has a highaffinity of with an5-HT serotonin receptor2A

of 397 nMKi


Hydroxy ziprasidoneCat No HY-100649

Hydroxy ziprasidone is an impurity of ZiprasidoneZiprasidone an antipsychotic agent is a combined5-HT (serotonin) and dopamine receptor antagonist


Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) Cat No HY-14338A

Idalopirdine Hydrochloride (Lu AE58054Hydrochloride) is a potent and selective 5-HT6

antagonist with a of 083 nMreceptor Ki


Iferanserin (S-MPEC) Cat No HY-118557

Iferanserin (S-MPEC) is a selective 5-HT ( ) antagonist with anreceptor serotonin receptor

affinity for Iferanserin has5-HT receptor2A

the potential for internal hemorrhoid diseasetreatment


Iloperidone (HP 873) Cat No HY-17410

Iloperidone (HP 873) is a receptorD 5-HT2 2

antagonist Iloperidone is an atypicalantipsychotic for the schizophrenia symptoms



Iloperidone hydrochloride (HP 873 hydrochloride) Cat No HY-17410A

Iloperidone hydrochloride (HP 873 hydrochloride)is a receptor antagonist IloperidoneD 5-HT2 2

hydrochloride is an atypical antipsychotic for theschizophrenia symptoms


Intepirdine (SB-742457 GSK-742457 RVT-101) Cat No HY-14339

Intepirdine (SB742457) is a highly selective 5-HT6receptor antagonist with pKi of 963 exhibitsgt100-fold selectivity over other receptors


IprindoleCat No HY-12392

Iprindole a tricyclic indole antidepressant is aweak inhibitor of the uptake of noradrenaline and5-HTltbrgt


Ipsapirone (TVX Q 7821 free base) Cat No HY-19686

Ipsapirone (TVX Q 7821) is an anxiolytic compoundand a receptor partial agonist5-HT1A

Ipsapirone (TVX Q 7821) also exhibits 5-HT1A

receptor antagonistic effect and only at highdoses it can also produce an inhibitory effect on5-HT and the α -adrenergic function2 1


Irindalone (Lu 21-098) Cat No HY-101632

Irindalone is a novel serotonin 5-HT2

antagonist


Isamoltane hemifumarateCat No HY-19578B

Isamoltane hemifumarate is a selective antagonistof with an of 39 nM for5-HT receptor1B IC50

inhibits the binding of [ I]ICYP to 5-HT1251B

recognition sites in rat brain membranesIsamoltane hemifumarate is also a β-adrenoceptorligand with an of 84 nMIC50


Isocorynoxeine (7-Isocorynoxeine) Cat No HY-N0775

Isocorynoxeine an isorhynchophylline-relatedalkaloid exhibits a dose-dependent inhibition of

receptor-mediated current response with5-HT2A

an of 724 μMIC50


IsopteropodineCat No HY-N4157

Isopteropodine is heteroyohimbine-type oxindolealkaloid components of Uncaria tomentosa(Willd) DC Isopteropodine acts as positivemodulators of and muscarinic M1 5-HT2receptors


JatrorrhizineCat No HY-N0749

Jatrorrhizine is an alkaloid isolatedfrom with neuroprotectiveCoptis chinensisantimicrobial antiplasmodial and antioxidantactivities


Jatrorrhizine chlorideCat No HY-N0740

Jatrorrhizine chloride is an alkaloid isolatedfrom with neuroprotectiveCoptis chinensisantimicrobial antiplasmodial and antioxidantactivities



Jatrorrhizine hydroxideCat No HY-N0749A

Jatrorrhizineensphydroxide is an alkaloid isolatedfrom with neuroprotectiveCoptis chinensisantimicrobial antiplasmodial and antioxidantactivities


JNJ-18038683Cat No HY-19889

JNJ-18038683 is a 5-Hydroxytryptamine Type 7( ) receptor antagonist with of 8195-HT7 pK si820 for rat and human 5-HT in HEK293 cells7

respectively


Ketanserin (R41468) Cat No HY-10562

Ketanserin is a selective 5-HT2 receptorantagonist Ketanserin also blocks hERG current( ) in a concentration-dependent mannerIhERG

( =011 μM)IC50


Ketanserin tartrate (R41468 tartrate) Cat No HY-10562A

Ketanserin (R41468) tartrate is a selective 5-HT2 antagonist Ketanserin tartrate alsoreceptor

blocks hERG current ( ) in aIhERG

concentration-dependent manner ( =011 μM)IC50


Keto ZiprasidoneCat No HY-100648

Keto Ziprasidone is an impurity of ZiprasidoneZiprasidone an antipsychotic agent is a combined5-HT (serotonin) and dopamine receptor antagonist


Latrepirdine dihydrochloride (Dimebolin dihydrochloride) Cat No HY-14537

Latrepirdine dihydrochloride is a neuroactivecompound with antagonist activity athistaminergic α-adrenergic and serotonergicreceptors Latrepirdine stimulates amyloidprecursor protein (APP) catabolism and

( ) secretionamyloid-β Aβ

Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Lesopitron dihydrochloride (E4424) Cat No HY-101609

Lesopitron dihydrochloride is a full and selective receptor agonist with of 125 nM in5-HT1A IC50

rat hippocampal membranes


Levomepromazine (Methotrimeprazine) Cat No HY-B1693

Levomepromazine (Methotrimeprazine) is an orallyavailable neuroleptic agent which is commonlyused to relieve nausea and vomiting in palliativecare settings


Lidanserin (ZK-33839) Cat No HY-101815

Lidanserin (ZK-33839) acts as a and5-HT2A

antagonistα -adrenergic receptor1

Purity gt980Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg

LintoprideCat No HY-U00121

Lintopride is a antagonist with moderate5HT45HT3 antagonist properties



LoxapineCat No HY-17390

Loxapine Succinate is a D2DR and D4DR inhibitorserotonergic receptor antagonist and also adibenzoxazepine anti-psychotic agent


Loxapine succinateCat No HY-17390A



LP-211Cat No HY-111455

LP-211 is a selective and bloodminusbrain barrierpenetrant agonist with a of5-HT receptor7 Ki

058 nM with high selectivity over 5-HT1A

receptor (K 188 nM) and D receptor (K 142 nM)i 2 i


Lumateperone tosylate (ITI-007 tosylate) Cat No HY-19733

Lumateperone tosylate (ITI-007 tosylate) is a5-HT2A receptor antagonist (Ki = 054 nM) apartial agonist of presynaptic D2 receptors and anantagonist of postsynaptic D2 receptors (Ki = 32nM) and a SERT blocker (Ki = 61 nM)


Lurasidone (SM-13496) Cat No HY-B0032A

Lurasidone (SM-13496) is an antagonist of both and with s of 168dopamine D2 5-HT7 IC50

and 0495 nM respectively Lurasidone (SM-13496)is also a partial agonist of receptor5-HT1A



Lurasidone Hydrochloride (SM-13496 Hydrochloride) Cat No HY-B0032

Lurasidone (Hydrochloride) (SM-13496(Hydrochloride)) is an antagonist of both

and with s of 168dopamine D2 5-HT7 IC50

and 0495 nM respectively

Purity 9987Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg 500 mg

LY 344864Cat No HY-13788

LY 344864 is a selective receptor agonist with anaffinity of 6 nM (Ki) at the recently cloned5-HT1F receptor IC50 Value 6 nM (Ki) Target5-HT1F LY 344864 possesses little affinity for the56 other serotonergic and non-serotonergicneuronal binding sites examined


LY 344864 hydrochlorideCat No HY-13788B

LY 344864 hydrochloride is a selective 5-HT1Fagonist with a of 6 nMKi


LY 344864 racemateCat No HY-13788C

LY 344864 racemate is a agonist5-HT receptor1F

extracted from patent US 5708187 A

Purity 9888Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

LY 344864 S-enantiomerCat No HY-13788A

LY 344864 S-enantiomer is the S-enantiomer ofLY344864 LY344864 is a 5-HT1F receptor agonist



LY310762Cat No HY-13527

LY310762 is a 5-HT1D receptor antagonist with Kiof 249 nM having a weaker affinity for 5-HT1Breceptor IC50 value 249 nM (Ki) Target 5-HT1Din vitro LY310762 has a higher affinity for theguinea pig 5-HT1D receptor than for the 5-HT1Breceptor


LY320135Cat No HY-W011040

LY320135 is a potent and selective antagonist of receptor with a of 141 nM LY320135 alsoCB1 Ki

binds to and with5-HT2 muscarinic receptorss of 64 μM and 21 μM respectively LY320135Ki

exhibits neuroprotective effect


LY334370Cat No HY-103107

LY334370 is a selective receptor agonist5-HT1F

with a of 16 nMKi


Masupirdine mesylate (SUVN-502 mesylate) Cat No HY-109118A

Masupirdine mesylate (SUVN-502 mesylate) is apotent selective orally bioavailable and brainpenetrant antagonist ( of 2045-HT6 receptor Ki

nM for human 5-HT6 receptor)

Purity gt98Clinical Data Phase 2Size 10 mM times 1 mL 1 mg

Melitracen hydrochlorideCat No HY-108256

Melitracen hydrochloride is an orally activebiphasic antidepressant and antianxiety agentMelitracen hydrochloride can inhibit the uptake ofNorepinephrine and through the5-HT (serotonin)presynaptic membrane inducing the increase ofmonoamine transmitters in synaptic space


MetergolineCat No HY-B1033

Metergoline is a psychoactive drug of the ergolinechemical class which acts as a ligand for variousserotonin and dopamine receptors


Methiothepin mesylate (Metitepine mesylate Ro 8-6837 mesylate) Cat No HY-107836

Methiothepin mesylate is a potent andnon-selective antagonist with5-HT receptor2

p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7

p s of 850 (5HT ) 868 (5HT ) andhellipKi 2A 2B

Purity 9932Clinical Data No Development ReportedSize 10 mg

Methylergometrine maleate (Methylergonovine maleate Ryegonovin Spametrin F) Cat No HY-100988

Methylergometrine maleate (Methylergonovinemaleate) is an ergot alkaloid and an activemetabolite of Methysergide with vasoconstrictiveand uterotonic activity


MHP 133Cat No HY-101653

MHP 133 is a drug with multiple CNS targets andinhibits acetylcholinesterase (AChE) with of 69Ki

μM also active against muscarinic M1 and M2receptors serotonin 5HT4 receptors and imidazoleI2 receptors


Mirtazapine (Org3770 6-Azamianserin) Cat No HY-B0352

Mirtazapine (Org3770) is a potent and orallyactive noradrenergic and specific serotonergicantidepressant (NaSSA) agent Mirtazapine is alsoa and5-HT2 5-HT3 histamine H1 receptor

antagonist with values ofα2-adrenoceptor pKi

805 81 93 and 695 respectively



Mirtazapine D3 (Org3770 D3 6-Azamianserin D3) Cat No HY-B0352S

Mirtazapine D3 (Org3770 D3 6-Azamianserin D3) isa deuterium labeled Mirtazapine Mirtazapine is a

inhibitor Mirtazapine is a potent5-HT receptorand orally active noradrenergic and specificserotonergic antidepressant (NaSSA) agent byblocking 5-HT2 and 5-HT3 receptors


ML 10302 hydrochlorideCat No HY-14442

ML 10302 hydrochloride is a potent and selective agonist with an of 45-HT receptor4 EC50

nMML 10302 hydrochloride displays more than680-fold selectivity over receptor in5-HT3

binding assay


Mosapride (TAK-370 AS-4370) Cat No HY-B0189

Mosapride is a gastroprokinetic agent that acts asa selective 5HT4 agonist Target 5HT4 Mosaprideis a gastroprokinetic agent that acts as aselective 5HT4 agonist


Mosapride citrate (TAK-370 citrate AS-4370 citrate) Cat No HY-B0189A

Mosapride citrate is a gastroprokinetic agent thatacts as a selective 5HT4 agonist Target 5HT4Mosapride is a gastroprokinetic agent that acts asa selective 5HT4 agonist


Myristicin (Myristicine) Cat No HY-N2510

Myristicine act as a serotonin receptorantagonist a weak monamine oxidase (MAO)inhibitor Myristicine is the main component ofnutmeg essential oil from Myristica

Houttfragrans


Naftidrofuryl oxalate (Nafronyl oxalate salt) Cat No HY-B1107

Naftidrofuryl oxalate (Nafronyl oxalate salt) is adrug used in the management of peripheral andcerebral vascular disorders as a vasodilatorenhance cellular oxidative capacity and may alsobe a 5-HT2 receptor antagonist


NAN-190 hydrobromideCat No HY-19818A

NAN-190 hydrobromide is a serotonin receptor 5-HTantagonist NAN-190 is a selective antagonist of

5-HT1A


Naratriptan (GR-85548A) Cat No HY-B0197

Naratriptan is a selective 5-HT1 receptor subtypeagonist and is a triptan drug that is used for thetreatment of migraine headaches Target 5-HT1Receptor Naratriptan is a triptan drug marketed byGlaxoSmithKline and is used for the treatment ofmigraine headaches


Naratriptan D3 Hydrochloride (GR-85548A D3) Cat No HY-B0197AS

Naratriptan D3 Hydrochloride is the deuteriumlabeled Naratriptan which is a selective 5-HT1receptor subtype agonist


Naratriptan hydrochloride (GR-85548A hydrochloride) Cat No HY-B0197A

Naratriptan hydrochloride is a selective 5-HT1receptor subtype agonist and is a triptan drugthat is used for the treatment of migraineheadaches



Nefazodone hydrochloride (BMY-13754 MJ-13754-1) Cat No HY-B1396

Nefazodone hydrochloride (BMY-13754) is a potentand selective ( =58 nM) antagonist with5HT2A Ki

moderate inhibition of 5-HT and noradrenalineuptake ( of 290 and 300 nM respectively)IC50


Nelotanserin (APD125) Cat No HY-10559

Nelotanserin is a potent inverse agonist5-HT2A

a moderately potent partial inverse5-HT2C

agonist and a weak inverse agonist with5-HT2B

of 17 79 791 nM in IP accumulationIC s50

assays respectively


Nemifitide diTFA (INN 00835 diTFA) Cat No HY-105077A

Nemifitide diTFA (INN 00835 diTFA) is a syntheticpentapeptide antidepressant with a potential forrapid onset of action Nemifitide diTFA is apeptide analog of melanocyte-inhibiting factor(MIF) Nemifitide diTFA can cross the blood-brainbarrier


NEO 376 (SPI-376) Cat No HY-101583

NEO 376 is a selective modulator of 5-HT1 and receptor GABA receptor dopamine with anti-psychotic activelyreceptor


Nexopamil racemateCat No HY-101727

Nexopamil racemate is the racemate of NexopamilNexopamil is a combined antagonistCa2+ 5-HT2

on thrombus formation in vivo and on plateletaggregation in vitro


NPS ALX Compound 4aCat No HY-103090

NPS ALX Compound 4a is a potent and selective5-hydroxytryptamine (5-HT ) receptor6 6

antagonist with an of 72 nM and a of 02IC50 Ki

nM


NRA-0160Cat No HY-101641

NRA-0160 is a selective dopamine D4 receptorantagonist with a value of 048 nM and withKi

negligible affinity for dopamine D2 receptor( gt10000 nM) ( 39 nM) ratKi D3 receptor Ki

( 180 nM) and rat 5-HT2A receptor Ki α1 ( 237 nM)adrenoceptor Ki


NuciferineCat No HY-N0049

Nuciferine is an antagonist at ( =4785-HT2A IC50

nM) ( =131 nM) and ( =15-HT2C IC50 5-HT2B IC50

μM) an inverse agonist at ( =150 nM)5-HT7 IC50

a partial agonist at ( =64 nM) D2 EC50 D5

( =26 μM) and ( =700 nM) anEC50 5-HT6 EC50

agonist at ( =32 μM) andhellip5-HT1A EC50


Ocaperidone (R79598) Cat No HY-101094

Ocaperidone is an effective antipsychotic agentacting as a potent and 5-HT2 dopamine D2

antagonist and a agonist with s of5-HT1A Ki

014 nM 046 nM 075 nM 16 nM and 54 nM for5-HT a -adrenergic receptor dopamine D 2 1 2

histamine H and a -adrenergichellip1 2


Olanzapine (LY170053) Cat No HY-14541

Olanzapine (LY170053) is a selective monoaminergicantagonist with high affinity binding to serotonin

( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki

nM respectively) ( =11 to 31dopamine D1-4 Ki

nM) ( =19-25 nM) andmuscarinic M1-5 Ki

( =19 nM)adrenergic α1 receptor Ki



Olanzapine D3 (LY170053 D3) Cat No HY-14541S

Olanzapine D3 (LY170053 D3) is the deuteriumlabeled Olanzapine


Ondansetron (GR 38032 SN 307) Cat No HY-B0002B

Ondansetron(GR 38032 SN 307) is a serotonin 5-HT3receptor antagonist used mainly as anantiemetic(to treat nausea and vomiting) often followingchemotherapy


Ondansetron hydrochloride (GR 38032 hydrochloride SN 307 hydrochloride) Cat No HY-B0002

Ondansetron hydrochloride (GR 38032 hydrochlorideSN 307 hydrochloride) is a serotonin 5-HT3receptor antagonist used mainly as anantiemetic(to treat nausea and vomiting) often followingchemotherapy


Ondansetron hydrochloride dihydrate (GR 38032 hydrochloride

dihydrate SN 307 hydrochloride dihydrate) Cat No HY-B0002A

Ondansetron hydrochloride dihydrate (GR 38032hydrochloride dihydrate SN 307 hydrochloridedihydrate) is a serotonin 5-HT3 receptorantagonist used mainly as anantiemetic (to treatnausea and vomiting) often followingchemotherapy

Purity 9987Clinical Data LaunchedSize 50 mg 100 mg 1 g 5 g

OPC-14523 free baseCat No HY-116594

OPC-14523 free base is an orally active sigmaand agonist with high affinity5-HT1A receptorfor sigma receptors (σ12 =4756 nM) theIC50

5-HT1A receptor ( =23 nM) and the 5-HTIC50

transporter ( =80 nM) OPC-14523 free baseIC50

shows antidepressant-like activity


OPC-14523 hydrochlorideCat No HY-116594A

OPC-14523 hydrochloride is an orally active and agonist with highsigma 5-HT1A receptor

affinity for sigma receptors (σ12 =4756 nM)IC50

the 5-HT1A receptor ( =23 nM) and the 5-HTIC50

transporter ( =80 nM) OPC-14523 hydrochlorideIC50



OpiranserinCat No HY-109067

Opiranserin a non-opioid and non-NSAID analgesiccandidate is a dual antagonist of glycine

and transporter type 2 (GlyT2) serotonin receptor 2A with s of 086 and 13 μM(5HT2A) IC50

respectively Opiranserin shows antagonisticactivity on rP2X3 (IC =087 μM)50


Org-12962Cat No HY-118152

Org-12962 is a potent selective and orally active agonist with a5-HT receptor2C

value of 701 Org-12962 also exhibitspEC50

high effacy for the 5-HT and 5-HT2A 2B

receptor with s of 638 and 628pEC50

respectively


Org-12962 hydrochlorideCat No HY-21994

Org 12962 hydrochloride is a potent selective andefficacious 5-HT receptor agonist and2C

exhibits values of 701 638 and 628pEC50

for 5-HT 5-HT and 5-HT 2C 2A 2A

respectively Org 12962 hydrochloride is effectivein panic-like anxiety animal modelltbrgt


OxatomideCat No HY-123205

Oxatomide is a potent and orally active dual and H1-histamine receptor P2X7 receptor

antagonist with antihistamine and anti-allergicactivity Oxatomide almost completely blocks theATP-induced current in human P2X7 receptors( of 095 μM)IC50



p-MPPI hydrochlorideCat No HY-120738

p-MPPI hydrochloride is a selective 5-HT1A antagonist with high affinity for 5-HT1Areceptor

receptors p-MPPI hydrochloride can crosses theblood-brain barrier and has clear antidepressantand anxiolytic-like effects


Paliperidone (9-Hydroxyrisperidone) Cat No HY-A0019

Paliperidone (9-Hydroxyrisperidone) the majoractive metabolite of Risperidone is a dopamine

antagonist and antagonistD2 5-HT2APaliperidone is also active as an antagonist at

and receptors andα1 α2 adrenergic receptorsH1-histaminergic


Paliperidone palmitate (9-Hydroxyrisperidone palmitate) Cat No HY-A0019A

Paliperidone palmitate (9-Hydroxyrisperidonepalmitate) an atypical long-acting antipsychoticagent is an ester prodrug of PaliperidonePaliperidone is a antagonist anddopamine

antagonist of the atypical antipsychotic5-HT2Aclass


PalonosetronCat No HY-A0018

Palonosetron is a 5-HT3 antagonist used in theprevention and treatment of chemotherapy-inducednausea and vomiting (CINV)


Palonosetron HydrochlorideCat No HY-A0021

Palonosetron Hcl is a 5-HT3 antagonist used in theprevention and treatment of chemotherapy-inducednausea and vomiting (CINV)


Pancopride (LAS 30451) Cat No HY-19684

Pancopride is a new potent and selective 5-HT3

antagonistreceptor


Pardoprunox (SLV-308 DU-126891) Cat No HY-14958

Pardoprunox (SLV-308) is a partial dopamine D2and partial agonist and a D3 receptor serotonin

agonist with s of 8 925-HT1A receptor pEC50

and 63 respectively


Pardoprunox hydrochloride (SLV-308 hydrochloride DU-126891 hydrochloride) Cat No HY-14958A

Pardoprunox (SLV-308) hydrochloride is a partial and partial agonistdopamine D2 D3 receptor

and a agonist withserotonin 5-HT1A receptors of 8 92 and 63 respectivelypEC50


Peptide 401Cat No HY-12537

Peptide 401 a potent mast cell degranulatingfactor from bee venom suppresses the increasedvascular permeability due to intradermal injectionof various smooth muscle spasmogens ( histamineand )5-HT

Purity 9829Clinical Data No Development ReportedSize 500 μg 1 mg 5 mg

Perospirone (SM-9018 free base) Cat No HY-B0731A

Perospirone (SM-9018 free base) is an orallyactive antagonist of receptor ( =06 nM)5-HT2A Ki

and receptor ( =14 nM) anddopamine D2 Ki

also a partial agonist of receptor5-HT1A

( =29 nM)Ki



Perospirone hydrochloride (SM-9018) Cat No HY-B0731

Perospirone hydrochloride (SM-9018) is an orallyactive antagonist of receptor ( of 065-HT2A Ki

nM) and receptor ( of 14 nM)dopamine D2 Ki

Perospirone hydrochloride is also a partialagonist of receptor ( of 29 nM)5-HT1A Ki


PerphenazineCat No HY-A0077

Perphenazine is a typical antipsychotic druginhibits 5-HT receptor Alpha-1A adrenergic2A

receptor Dopamine receptor D2D3 D2L receptorand with values ofHistamine H1 receptor Ki

56 10 0765013 34 and 8 nM respectively


Perphenazine D8 DihydrochlorideCat No HY-A0077AS

Perphenazine D8 Dihydrochloride is the deuteriumlabeled Perphenazine which is a typicalantipsychotic drug(5-HT Dopamine receptorligand)


PF-04995274Cat No HY-18137

PF-04995274 is a potent high-affinity orallyactive and partial serotonin 4 receptor (5-HT R)4

agonist


Phenylbiguanide (N-Phenylbiguanide PBG 1-Phenylbiguanide) Cat No HY-101331

Phenylbiguanide is a selective5-HT receptor3

agonist with an of 30plusmn01 μMEC50


Piboserod (SB-207266) Cat No HY-15574

Piboserod (SB 207266) is a selective 5-HT(4)receptor antagonist IC50 value Target 5-HT4antagonist in vitro Piboserod did not modify thebasal contractions but concentration-dependentlyantagonized the ability of 5-HT to enhance bladderstrip contractions to EFS


Piboserod hydrochloride (SB-207266 hydrochloride) Cat No HY-15574A

Piboserod (SB 207266) Hcl is a selective 5-HT(4)receptor antagonist IC50 value Target 5-HT4antagonist in vitro Piboserod did not modify thebasal contractions but concentration-dependentlyantagonized the ability of 5-HT to enhance bladderstrip contractions to EFS


Pimavanserin (ACP-103) Cat No HY-14557

Pimavanserin is a selective inverse agonist of the receptor with and of 873 and5-HT2A pIC50 pKd

93 respectively


Pimavanserin tartrate (ACP-103 tartrate) Cat No HY-14557A

Pimavanserin tartrate (ACP-103) is a potent 5-HT receptor inverse agonist with and of2A pIC50 pKi

873 and 93 respectively


Pimethixene (Pimetixene) Cat No HY-B1101

Pimethixene is antihistamine and antiserotonergiccompound acts as an antimigraine agent



Pimethixene maleate (Pimetixene maleate) Cat No HY-B1101A

Pimethixene maleate is antihistamine andantiserotonergic compound acts as an antimigraineagent


Pindolol (LB-46) Cat No HY-B0982

Pindolol (LB-46) is a nonselective β-blocker withpartial beta-adrenergic receptor agonist activityalso functions as a 5-HT1A receptor weak partialantagonist (Ki=33nM)


Pipamperone (Floropipamide McN-JR 3345 R 3345) Cat No HY-100703

Pipamperone (Floropipamide McN-JR 3345 R 3345)is a high-affinity antagonist of 5-HT2A

( =82) and ( =80)receptor pKi D receptor4 pKi

and a low-affinity antagonist of D receptor2

(pK =67)i

Purity 9989Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg

Piromelatine (Neu-P11) Cat No HY-105285

Piromelatine (Neu-P11) is a melatonin receptor agonist MT MT1 2 serotonin

agonist and 5-HT1A 5-HT1D serotonin 5-HT2B

antagonist


Pizotifen (Pizotyline BC-105) Cat No HY-B0115

Pizotifen (Pizotyline) is a potent 5-HT2

receptor antagonist with a high affinity for binding site5-HT1C


Pizotifen malate (Pizotyline malate BC-105 malate) Cat No HY-B0115A

Pizotifen malate (Pizotyline malate) is a potent receptor antagonist with a high affinity5-HT2

for binding site5-HT1C


PNU-142633Cat No HY-103131

PNU-142633 is a high affinity selective andorally active agonist with s5-HT receptor1D Ki

of 6 nM and gt 18 000 nM for human 5-HT1D

and human 5-HT receptorreceptor 1B

respectively PNU-142633 has anti-migraineefficacy


PrucaloprideCat No HY-14151

Prucalopride (R093877) is a drug acting as aselective high affinity 5-HT4 receptoragonist(pKi=8681 for 5-HT4a4b) gt150-foldhigher affinity for 5-HT4 receptors than for otherreceptors


Prucalopride succinate (R-108512) Cat No HY-12694

Prucalopride succinate is a selective highaffinity 5-HT4 receptor agonist with pKi of8681 for 5-HT4a4b


PRX-08066Cat No HY-15472

PRX-08066 is a selective 5-hydroxytryptaminereceptor 2B (5-HT2BR IC50= 34 nM) antagonistthat causes selective vasodilation of pulmonaryarteries



PU02Cat No HY-103118

PU02 a derivative of 6-MP (HY-13677) is anegative allosteric modulator (NAM) of 5-HT3

with values of 036 and 073 μM inreceptor IC50

HEK293 cells transfected with human 5-HT A and3

5-HT AB receptors respectively3


PuerarinCat No HY-N0145

Puerarin an isoflavone extracted from Radix is a receptor antagonistpuerariae 5-HT2C


Pumosetrag Hydrochloride (MKC-733 DDP-733) Cat No HY-19650

Pumosetrag Hydrochloride (MKC-733 DDP-733) is anorally available partial agonist developed5-HT3for the treatment of irritable bowel syndrome andgastroesophageal reflux disease


Quetiapine (ICI204636) Cat No HY-14544

Quetiapine (ICI204636) is a 5-HT receptorsagonist with a of 477 for human 5-HT1ApEC50

receptor Quetiapine is a dopamine receptorantagonist with a of 633 for human D2pIC50

receptor


Quetiapine D4 fumarateCat No HY-B0031S

Quetiapine D4 fumarate is the deuterium labeledQuetiapine fumarate Quetiapine fumarate is a 5-HTreceptors agonist and a dopamine receptorantagonist Antidepressant and anxiolytic effects


Quetiapine D4 hemifumarateCat No HY-B0031S1

Quetiapine D4 hemifumarate is the deuteriumlabeled Quetiapine hemifumarate Quetiapinehemifumarate is a 5-HT receptors agonist and adopamine receptor antagonist Antidepressant andanxiolytic effects


Quetiapine hemifumarateCat No HY-B0031

Quetiapine hemifumarate is a 5-HT receptorsagonist with a of 477 for human 5-HT1ApEC50

receptor Quetiapine hemifumarate is a dopamine antagonist with a of 633 forreceptor pIC50

human D2 receptor


R 59-022 (DKGI-I Diacylglycerol kinase inhibitor I) Cat No HY-107613

R 59-022 (DKGI-I) is a diacylglycerol kinaseinhibitor ( =28 μM) R 59-022 is a IC50 5-HTRantagonist and activates protein kinase C (PKC)


Ramosetron Hydrochloride (YM060) Cat No HY-B0595

Ramosetron Hydrochloride(YM060 Hydrochloride) is aserotonin 5-HT3 receptor antagonist for thetreatment of nausea and vomiting Target 5-HT3Receptor Ramosetron hydrochloride selectivelyblocks serotonin receptors (5-HT3)


RevexeprideCat No HY-U00373

Revexepride is a highly selective 5-HT4 receptoragonist and a potential inducer of CYP3A4

used for the treatment ofenzymegastroesophageal reflux disease



RG-12915Cat No HY-19110

RG-12915 is a selective antagonist with5-HT3 value of 016 nMIC50


Risperidone (R 64 766) Cat No HY-11018

Risperidone is a serotonin 5-HT receptor2

blocker inhibitor and potentP-Glycoprotein antagonist with ofdopamine D receptor2 K si

48 59 nM for 5-HT and dopamine D receptor2A 2

respectively


Risperidone hydrochloride (R 64 766 hydrochloride) Cat No HY-11018A

Risperidone hydrochloride (R 64 766 hydrochloride) blocker inhibitor5-HT receptor2 P-Glycoprotein

and potent antagonistdopamine D receptor2

with of 48 59 nM for 5-HT and dopamineK si 2A

D receptor respectively2


Risperidone mesylate (R 64 766 mesylate) Cat No HY-11018B

Risperidone mesylate(R 64 766 mesylate) is aserotonin blocker 5-HT receptor2 P-Glycoproteininhibitor and potent dopamine D receptor2

antagonist with of 48 59 nM for 5-HTK si 2A

and dopamine D receptor respectively2


Ritanserin (R 55667) Cat No HY-10791

Ritanserin (R 55667) is a highly potentrelatively selective orally active long actingantagonist of with an of5-HT receptor2 IC50

09 nM less active on Histamine H Dopamine1

D Adrenergic α Adrenergic α receptors2 1 2


Rizatriptan benzoate (MK 462) Cat No HY-B0206

Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonisttriptan drug for the treatment of migraineheadaches Target 5-HT1 agonist RizatriptanBenzoate(Maxalt) is a 5-HT1 agonist triptan drugfor the treatment of migraine headaches


Ro 04-6790Cat No HY-14335

Ro 04-6790 is a potent competitive and selective receptor antagonist with values of5-HT6 pKi

726 735 for rat and human 5-HT6 receptorsrespectively Ro 04-6790 has no affinity at otherreceptors


Roluperidone (CYR-101 MIN-101 MT-210) Cat No HY-19469

Roluperidone (CYR-101) is a novel cyclic amidederivative that has high equipotent affinities for

and receptors ( of 753 nM5-HT2A sigma-2 Ki

and 819 nM for 5-HT and sigma-22A

respectively)


Rotigotine (N-0437 N-0923) Cat No HY-75502

Rotigotine (N-0437 N-0923) is a full agonist of a partial agonist of thedopamine receptor

and an antagonist of the5-HT1A receptor with s of 071nMα2B-adrenergic receptor Ki

4-15nM and 83nM for the dopamine D3 receptorand D2 D5 D4 receptors and dopaminehellip


Rotigotine Hydrochloride (N-0923 Hydrochloride) Cat No HY-A0007

Rotigotine Hydrochloride (N-0923 Hydrochloride) isa full agonist of a partialdopamine receptoragonist of the and an5-HT1A receptorantagonist of the with α2B-adrenergic receptor Ki

of 071nM 4-15nM and 83nM for the dopamine D3receptor and D2 D5 D4 receptors and dopaminehellip



Rotundine ((-)-Tetrahydropalmatine L-Tetrahydropalmatine) Cat No HY-N0096

Rotundine is an antagonist of dopamine D1 D2and with s of 166 nM 14 μMD3 receptors IC50

and 33 μM respectively Rotundine is also anantagonist of with an of 370 nM5-HT1A IC50


RS-127445Cat No HY-15419A

RS-127445 is a selective high affinity orallybioavailable antagonist with a5-HT receptor2B

of 95 RS-127445 shows 1000 fold selectivitypKi

for this receptor as compared to numerous otherreceptor and ion channel binding sites


RS-127445 hydrochlorideCat No HY-15419

RS-127445 hydrochloride is a selective highaffinity orally bioavailable 5-HT receptor2B

antagonist with a of 95 RS-127445pKi

hydrochloride shows 1000 fold selectivity for thisreceptor as compared to numerous other receptorand ion channel binding sites


RU 24969Cat No HY-16688

RU 24969 is a preferential agonist with5-HT1B

a of 038 nM but also displays appreciableKi

affinity for the ( =25 nM)5-HT receptor1A Ki

and has low affinity for other receptor sites inthe brain RU 24969 could decrease fluidconsumption and increase forward locomotion


RU 24969 hemisuccinateCat No HY-16688B

RU 24969 hemisuccinate is a preferential 5-HT1B

agonist with a of 038 nM but also displaysKi

appreciable affinity for the 5-HT receptor1A

( =25 nM) and has low affinity for otherKi

receptor sites in the brain


Sarpogrelate hydrochloride (MCI-9042) Cat No HY-10564

Sarpogrelate hydrochloride (MCI-9042) is aselective antagonist with s of 8525-HT R2 pKi

657 and 743 for 5-HT 5-HT and 5-HT2A 2B 2C

receptors respectively


SB 242084Cat No HY-13409

SB 242084 is a 5-HT2C receptor antagonist(pKi=90)that displays 158- and 100-fold selectivity over5-HT2A and 5-HT2B receptors respectively


SB 242084 hydrochlorideCat No HY-13409A

SB 242084 hydrochloride is a 5-HT2C receptorantagonist(pKi=90) that displays 158- and100-fold selectivity over 5-HT2A and 5-HT2Breceptors respectively


SB 243213Cat No HY-103112B

SB 243213 is an orally active selective andhigh-affinity antagonist with a5-HT receptor2C

of 937 and a of 98 for human 5-HTpKi pKb 2C

receptor SB 243213 shows greater than a 100-foldselectivity over a wide range of neurotransmitterreceptors enzymes and ion channels


SB 243213 dihydrochlorideCat No HY-103112A

SB 243213 dihydrochloride is an orally activeselective and high-affinity 5-HT receptor2C

antagonist with a of 937 and a of 98pKi pKb

for human 5-HT receptor2C



SB 243213 hydrochlorideCat No HY-103112

SB 243213 hydrochloride is an orally activeselective and high-affinity 5-HT receptor2C



Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

SB 258719Cat No HY-U00443

SB 258719 is a selective 5-HT receptor7

antagonist with a of 75pKi


SB 271046 Hydrochloride (SB 271046A) Cat No HY-14336A

SB 271046 Hydrochloride (SB 271046A) is a potentselective and orally active 5-HT6 receptorantagonist with of 902 855 and 881 forpKi

rat pig and human respectively


SB-200646Cat No HY-103129A

SB-200646 is the first selective over5-HT2B2C

5-HT receptor antagonist with values of2A pKi

75 69 and 52 for and5-HT2B 5-HT2C

5-HT respectively SB-200646 is orally active2A

and has electrophysiological and anxiolyticproperties in vivo


SB-200646ACat No HY-103129

SB-200646A is the first selective over5-HT2B2C



5-HT respectively SB-200646A is orally active2A



SB-215505Cat No HY-18596

SB-215505 is a potent and subtype-selective receptor antagonist with values of5-HT2B pKi

83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C

respectively SB-215505 increases wakefulness andmotor activity in rats


SB-224289 hydrochloride (SB-224289A) Cat No HY-101105A

SB-224289 hydrochloride is a selective 5-HT1B antagonist with anxiolytic effectreceptor


SB-269970Cat No HY-15370

SB269970 is a antagonist with 5-HT7 receptor pKiof 83 exhibits gt50-fold selectivity againstother receptors



SB269970 hydrochloride (SB-269970A) is ahydrochloride salt form of SB-269970 which is a

antagonist with the of 835-HT7 receptor pKi

exhibits gt50-fold selectivity against otherreceptors


SB-277011 hydrochloride (SB-277011A hydrochloride) Cat No HY-10847B

SB-277011 hydrochloride (SB-277011A hydrochloride)is a potent selective orally bioavailable andbrain penetrate dopamine D receptor3

antagonist with values of(D R)3 Ki

107 nM and 112 nM at rodentand human D R respectively3



SB-399885 hydrochlorideCat No HY-103099

SB-399885 hydrochloride is a 5-HT receptor6

antagonist


SB-616234-ACat No HY-19477

SB-616234-A is a selective and orally bioavailable antagonist with anxiolytic and5-HT1B receptor

antidepressant activity


SB228357Cat No HY-103154

SB228357 is a selective potent and orall active antagonist with values5-HT receptor2C2B pKi

of 69 80 and 90 for and5-HT2A 5-HT2B

respectively SB228357 has5-HT2C

antidepressantanxiolytic effects


SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) Cat No HY-19545A

SCH-23390 hydrochloride (R-(+)-SCH-23390hydrochloride) is a potent and selective

antagonist with sdopamine D -like receptor1 Ki

of 02 nM and 03 nM for the and D1 D5

respectivelyreceptor


SCH-23390 maleate (R-(+)-SCH-23390 maleate) Cat No HY-108400

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is apotent and selective dopamine D -like receptor1

antagonist with s of 02 nM and 03 nM for theKi

and respectivelyD1 D receptor5


SEP-363856 hydrochloride (SEP-856 hydrochloride) Cat No HY-136109

SEP-363856 hydrochlorideSEP-856 hydrochloridean orally active and CNS active psychotropic agentwith a unique non-D25-HT2A mechanism of actionexerts its antipsychotic-like effects SEP-363856hydrochlorideSEP-856 hydrochloride has thepotential for the treatment of schizophrenia


Serotonin hydrochloride (5-Hydroxytryptamine hydrochloride 5-HT hydrochloride) Cat No HY-B1473

Serotonin hydrochloride is a monoamineneurotransmitter in the CNS and an endogenous

agonist Serotonin hydrochloride5-HT receptoris also a ( )catechol O-methyltransferase COMTinhibitor with a of 44 μMKi


Sertindole (Lu 23-174) Cat No HY-14543

Sertindole a neuroleptic is one of the newerantipsychotic medications available TargetMulti-target In vitro studies showed thatsertindole exerts a potent antagonism at serotonin5-HT2A 5-HT2C dopamine D2 and αl adrenergicreceptors


Setiptiline (Org-8282) Cat No HY-32329

Setiptiline (Org-8282) is a serotonin receptorantagonist Setiptiline is a tetracyclicantidepressant (TeCA) which acts as anoradrenergic and specific serotonergicantidepressant (NaSSA)


Setiptiline maleate (MO-8282) Cat No HY-32329A

Setiptiline (MO-8282) is a serotonin receptorantagonist Setiptiline is a tetracyclicantidepressant (TeCA) which acts as anoradrenergic and specific serotonergicantidepressant (NaSSA)



SKF-83566Cat No HY-103430A

SKF-83566 is a potent blood-brain permeableand orally active D1-like dopamine receptor

antagonist and a weaker competitive(D1DR)antagonist at the vascular 5-HT receptor2

( =11 nM)Ki


SKF-83566 hydrobromideCat No HY-103430

SKF-83566 hydrobromide is apotent blood-brain permeable and orallyactive D1-like dopamine receptor


( =11 nM)Ki


Spiperone hydrochloride (Spiroperidol hydrochloride) Cat No HY-B1371A

Spiperone hydrochloride (Spiroperidolhydrochloride) is a selective dopamine D2

( values of 006 nM 06 nM 008 nMreceptor Ki

~350 nM ~3500 nM for D D D and DD2 3 4 1 5

receptors respectively) and 5-HT 5-HT2A 1A

( s of 1 nM49 nM)hellipreceptor Ki


Spiramide (AMI-193) Cat No HY-100971

Spiramide (AMI-193) is a potent and selectiveantagonist of and 5-HT2 dopamine D2

with s of 2 nM and 3 nMreceptor Ki

respectively Spiramide has gt2000-foldselectivity for 5-HT versus ( =43002 5-HT1C Ki

nM) receptors


SR 57227ACat No HY-102064

SR 57227A is a potent orally active and selective agonist with ability to cross5-HT3 receptor

the blood brain barrier


Strictosidinic acidCat No HY-N7514

Strictosidinic acid an orally active glycosideindole monoterpene alkaloid isolated from

leaves inhibits precursorPsychotria myrianthaenzymes of biosynthesis and reduces the 5-HT5-HTlevels Strictosidinic acid has peripheralanalgesic and antipyretic activities in mice


Sulamserod (RS-100302) Cat No HY-101668

Sulamserod is a antagonist with5-HT4 receptorantiarrhythmic activities


Sumatriptan succinate (GR 43175) Cat No HY-B0121

Sumatriptan succinate (GR 43175) is a serotonin1(5-HT1) receptor agonist which is effective inthe acute treatment of migraine headache


Syk Inhibitor IICat No HY-112390A

Syk Inhibitor II is a potent high selective andATP-competitive inhibitor with an of 41Syk IC50

nM Syk Inhibitor II inhibits release from5-HTRBL-cells with an of 460 nM Syk Inhibitor IIIC50

shows less potent against other kinases and hasanti-allergic effect


T 82Cat No HY-U00028

T 82 is a potent antagonist and5-HT3 inhibitor used foracetylcholinesterase (AChE)

treatment of Alzheimers Disease



Talipexole dihydrochloride (B-HT 920 dihydrochloride) Cat No HY-A0008

Talipexole dihydrochloride (B-HT 920dihydrochloride) is a dopamine D2 receptoragonist α2-adrenoceptor agonist and 5-HT3receptor antagonist which displaysantiParkinsonian activity


Tandospirone (SM-3997) Cat No HY-14558

Tandospirone (SM-3997) is a potent and selective receptor partial agonist with a of 275-HT1A Ki

nM Tandospirone can be used for the research ofthe central nervous system disorders and theunderlying mechanisms


Tandospirone citrate (SM-3997 citrate) Cat No HY-B0061

Tandospirone citrate is a potent and selective5-HT1A receptor partial agonist (Ki = 27 nM) thatdisplays selectivity over SR-2 SR-1C α1 α2 D1and D2 receptors (Ki values ranging from1300-41000 nM)


Tegaserod maleate (SDZ-HTF-919 HTF-919) Cat No HY-14153A

Tegaserod maleate is a selective receptor5-HT4

partial agonist and a receptor5-HT2B

antagonist Tegaserod maleate exhibits a promotileeffect throughout the gastrointestinal (GI) tract


Temanogrel (APD791) Cat No HY-10560

Temanogrel is a highly selective 5-HT2A


Purity 9894Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Tertatolol ((plusmn)-Tertatolol Racemic Tertatolol dl-Tertatolol) Cat No HY-U00356

Tertatolol is a potent antagonist of and withbeta-adrenoceptor 5-HT receptor

unique renal vasodilatatory effects


TG6-10-1Cat No HY-16978

TG6-10-1 is an antagonist showsEP2low-nanomolar antagonist activity against onlyEP2 gt300-fold selectivity over human EP3 EP4and IP receptors 100-fold selectivity over EP1receptors


Thioridazine hydrochlorideCat No HY-B0965

Thioridazine hydrochloride is an antipsychoticdrug used in the treatment of schizophrenia andpsychosis shows D4 selectivity or serotoninantagonism


TianeptineCat No HY-90003

Tianeptine is a selective facilitator of 5-HTuptake Tianeptine has no affinity for a widerange of receptors including 5-HT and dopamine(IC gt10 μM) and has no effect on noradrenalin50

or dopamine uptake


Tianeptine sodium saltCat No HY-90003A

Tianeptine sodium salt is a selective facilitatorof uptake Tianeptine sodium salt has no5-HTaffinity for a wide range of receptors including5-HT and dopamine (IC gt10 μM) and has no effect50

on noradrenalin or dopamine uptake



TIK-301 (PD-6735 LY-156735) Cat No HY-106136

TIK-301 (PD-6735) is a chlorinated melatoninderivative and a potent high-affinity and orallyactive and melatonin MT1 MT receptors2

agonist with s of 0081 nM and 0042 nMKi

respectively


Trazodone hydrochloride (AF-1161) Cat No HY-B0478

Trazodone (hydrochloride) (AF-1161) is anantidepressant belonging to the class of serotoninreceptor antagonists and reuptake inhibitors fortreatment of anxiety disorders


Trimipramine maleateCat No HY-B1213

Trimipramine maleate is a 5-HT receptorantagonist with pK s of 639 810 466 fori

5-HT 5-HT and 5-HT respectively1C 2 1A


Tropisetron (SDZ-ICS-930 free base) Cat No HY-B0072

Tropisetron (SDZ-ICS-930 free base) is a selective5-HT3 receptor antagonist and α7-nicotinicreceptor agonist with an IC50 of 701 plusmn 09 nM for5-HT3 receptor


Tropisetron Hydrochloride (SDZ-ICS-930) Cat No HY-B0020

Tropisetron Hydrochloride (SDZ-ICS-930) is aselective 5-HT3 receptor antagonist andα7-nicotinic receptor agonist with an IC50 of 701plusmn 09 nM for 5-HT3 receptor


UrapidilCat No HY-B0716

Urapidil is an antagonist andα1 adrenoreceptora agonist5-HT receptor1A


Urapidil D6Cat No HY-B0716S

Urapidil D6 is a deuterium labeled UrapidilUrapidil is an antagonist and aα1-adrenoreceptor

agonist5-HT receptor1A


Urapidil hydrochlorideCat No HY-B0354A

Urapidil HCl is an α1-adrenoceptor antagonist and5-HT1A receptor agonist


Vabicaserin hydrochloride (SCA 136) Cat No HY-111200

Vabicaserin hydrochloride is a 5-hydroxytryptamine2C ( ) -selective agonist with an5-HT2C receptor

of 8 nMEC50


Vilazodone (EMD 68843 SB659746A) Cat No HY-14262

Vilazodone (EMD 68843 SB 659746A) is a potentselective and orallyactive serotonin reuptake inhibitor (SSRI)and partial agonist5-HT A receptor1



Vilazodone Hydrochloride (EMD 68843 Hydrochloride SB659746A Hydrochloride) Cat No HY-14261

Vilazodone Hydrochloride (EMD 68843 Hydrochloride)is a transporter (SER) inhibitor andserotonin

receptor partial agonist5-HT1A


Volinanserin (MDL100907 M 100907) Cat No HY-14940

Volinanserin is a potent and selective antagonistof with a of 036 nM and5-HT receptor2 Ki

shows 300-fold selectivity for 5-HT receptor2

over 5-HT alpha-1 and DA D receptors1c 2

Volinanserin has antipsychotic activity


Vortioxetine (Lu AA 21004) Cat No HY-15414

Vortioxetine is a inhibitor of 5-HT 5-HT 1A 1B

receptor and with 5-HT 5-HT3A 7 SERT Ki

values of 15 nM 33 nM 37 nM 19 nM and 16 nMrespectively

Purity 9952Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Vortioxetine D8 (Lu AA 21004 D8) Cat No HY-15414S

Vortioxetine D8 is a deuterium labeledVortioxetine Vortioxetine is an inhibitor of

receptor and5-HT 5-HT 5-HT 5-HT1A 1B 3A 7

with values of 15 nM 33 nM 37 nM 19SERT Ki

nM and 16 nM respectively


Vortioxetine hydrobromide (Lu AA21004 hydrobromide) Cat No HY-15414A

Vortioxetine hydrobromide is a multimodalserotonergic agent inhibits 5-HT 5-HT 1A 1B

receptor and with values5-HT 5-HT3A 7 SERT Ki

of 15 nM 33 nM 37 nM 19 nM and 16 nMrespectively

Purity 9994Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

WAY-100635Cat No HY-10349

WAY-100635 is a potent and selective 5-HT1A

Receptor antagonist with a pIC of 887 an50

apparent pA of 971 WAY-100635 is a potent and2

selective 5-hydroxytryptamine 1A (5-HT1A) antagonist with an value of 091 nMreceptor IC50

and value of 039 nMKi


WAY-100635 MaleateCat No HY-10349A

WAY-100635 maleate is a potent and selective5-hydroxytryptamine 1A (5-HT1A) receptorantagonist with an value of 091 nM and IC50 Ki

value of 039 nM WAY-100635 maleate has pIC50

values for and α1-adrenergic receptors of5-HT1A89 and 66 respectively

Purity gt980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg

WAY-181187 (SAX-187) Cat No HY-14340

WAY-181187 (SAX-187) is a potent and selectivefull receptor agonist with a of 22 nM5-HT6 Ki

and an of 66 nM WAY181187 mediates 5-HT6EC50

receptor-dependent signal pathways such as cAMPFyn and ERK12 kinase as specific agonist


Xaliproden hydrochloride (SR57746A SR57746 hydrochloride) Cat No HY-14604

Xaliproden hydrochloride (SR57746A) is a potentselective and orally active agonist of 5-HT1A

shows a high affinity for 5-HTreceptor 1A

specific binding sites in the rat hippocampus( =3 nM)IC50


Xanthotoxol (8-Hydroxypsoralen) Cat No HY-30152

Xanthotoxol (8-Hydroxypsoralen) is a biologicallyactive linear furocoumarin shows strongpharmacological activities as anti-inflammatoryantioxidant antagonistic and5-HTneuroprotective effects



YL0919Cat No HY-100769

YL0919 is an orally active antidepressant agentwith dual activity as a highly seletive 5-HT

blocker and an effectiveuptake agonist ( =019 nM)5-HT receptor1A Ki


Zatosetron maleate (LY 277359 maleate) Cat No HY-U00234

Zatosetron maleate is a potent and selective 5HT3 antagonistreceptor


Ziprasidone (CP-88059) Cat No HY-14542

Ziprasidone an antipsychotic agent is a combined and 5-HT (serotonin) dopamine receptor

antagonist Ziprasidone has high affinity for rat( 34 nM)human (25 nM) 5-HT1A receptorsKi

5-HT2A (042 nM) and dopamine D2 receptors (48nM)


Ziprasidone amino acid (Ziprasidone Impurity C Ziprasidone open ring impurity) Cat No HY-131255

Ziprasidone amino acid (Ziprasidone Impurity C) isan impurity of Ziprasidone Ziprasidone is acombined and 5-HT (serotonin) dopamine

antagonist Ziprasidone exhibits potentreceptoreffects of antipsychotic activity


Ziprasidone hydrochloride (CP-88059 hydrochloride) Cat No HY-14542A

Ziprasidone (CP-88059) hydrochloride anantipsychotic agent is a combined 5-HT

and antagonist(serotonin) dopamine receptor


Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) Cat No HY-17407

Ziprasidone (CP 88059) hydrochloride monohydratean antipsychotic agent is an orally activecombined and 5-HT (serotonin) dopamine

antagonistreceptor



5-HT Receptor Antagonists Agonists Inhibitors Modulators amp Activators

(4E)-SUN9221Cat No HY-U00367

(4E)-SUN9221 is a potent antagonist of and withα1-adrenergic receptor 5-HT2 receptor

antihypertensive and anti-platelet aggregationactivities


(R)-Mirtazapine ((R)-Org3770 (R)-6-Azamianserin) Cat No HY-B0352B

(R)-Mirtazapine ((R)-Org3770) is a R(minus)-enantiomerof Mirtazapine with antinociceptive properties inan animal model of acute thermal nociception(R)-Mirtazapine is a antagonist5-HT receptor3

(R)-Mirtazapine is mainly metabolized by CYP3A4


(R)-Mirtazapine D3 ((R)-Org3770 D3 (R)-6-Azamianserin D3) Cat No HY-B0352BS

(R)-Mirtazapine D3 ((R)-Org3770 D3) is a deuteriumlabeled (R)-Mirtazapine (R)-Mirtazapine is aR(minus)-enantiomer of Mirtazapine withantinociceptive properties in an animal model ofacute thermal nociception (R)-Mirtazapine is a



(R)-Praziquantel D11Cat No HY-126057S

(R)-Praziquantel D11 is the deuterium labeled(R)-Praziquantel (R)-Praziquantel the activeenantiomer of Praziquantel is a partial agonistof the human 5-HT2B receptor (R)-Praziquantelacts as an antischistosomal eutomer


(RR)-Palonosetron HydrochlorideCat No HY-A0021C

(RR)-Palonosetron Hydrochloride is the activeenantiomer of Palonosetron


(Rac)-Rotigotine hydrochlorideCat No HY-15394

(Rac)-Rotigotine hydrochloride is a racemate ofRotigotine


(Rac)-WAY-161503Cat No HY-103138A

(Rac)-WAY-161503 is a potent selective highlyaffinity agonist with a of 45-HT receptor2C Ki

nM and an EC of 12 nM (Rac)-WAY-16150350

displays higher affinity for 5-HT than 5-HT2C 2A

and 5-HT receptors (Rac)-WAY-161503 has2B

anti-obesity and antidepressant effects


(S)-Mirtazapine ((S)-Org3770 (S)-6-Azamianserin) Cat No HY-B0352A

(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomerof Mirtazapine with pronociceptive properties inan animal model of acute thermal nociception(S)-Mirtazapine is a stereoselective 5-HT2

antagonist (S)-Mirtazapine isreceptormetabolized by CYP2D6 and CYP1A2


(S)-Mirtazapine D3 ((S)-Org3770 D3 (S)-6-Azamianserin D3) Cat No HY-B0352AS

(S)-Mirtazapine D3 ((S)-Org3770 D3) is a deuteriumlabeled (S)-Mirtazapine (S)-Mirtazapine is aS(+)-enantiomer of Mirtazapine with pronociceptiveproperties in an animal model of acute thermalnociception(S)-Mirtazapine is a stereoselective



(Z)-ThiothixeneCat No HY-108324

(Z)-Thiothixene is an antagonist of serotonergic extracted from patent US 20150141345 A1receptor




























of 18 μMKi

















blocking activity








































542) 5-HT (pIC lt5)50













































































AR-A 2 (AR-A 000002) Cat No HY-107018





















( s = 897 nM 490 nM 66 nM and 985 nMKi

respectively)







of 84-105 89-95 89-94 andhellip













































antipsychotic





antipsychotic






nM










modulator(5-HT)






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor




























of 18 μMKi

















blocking activity








































542) 5-HT (pIC lt5)50













































































AR-A 2 (AR-A 000002) Cat No HY-107018





















( s = 897 nM 490 nM 66 nM and 985 nMKi

respectively)







of 84-105 89-95 89-94 andhellip













































antipsychotic





antipsychotic






nM










modulator(5-HT)






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor








































542) 5-HT (pIC lt5)50













































































AR-A 2 (AR-A 000002) Cat No HY-107018





















( s = 897 nM 490 nM 66 nM and 985 nMKi

respectively)







of 84-105 89-95 89-94 andhellip













































antipsychotic





antipsychotic






nM










modulator(5-HT)






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor










































AR-A 2 (AR-A 000002) Cat No HY-107018





















( s = 897 nM 490 nM 66 nM and 985 nMKi

respectively)







of 84-105 89-95 89-94 andhellip













































antipsychotic





antipsychotic






nM










modulator(5-HT)






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor
















( s = 897 nM 490 nM 66 nM and 985 nMKi

respectively)







of 84-105 89-95 89-94 andhellip













































antipsychotic





antipsychotic






nM










modulator(5-HT)






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor























antipsychotic





antipsychotic






nM










modulator(5-HT)






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor






















( =26 nM)Ki




( =0085 nM) and ( =049 nM)D3 Ki D2 Ki















respectively







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor







of 3500 nM)





respectively5-HT2A











5-HT receptors2A































stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor













stimulatory agonist
















respectively














activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor








activity





of 114 nMKd





patent WO 2005002578 A1





F-15599 (NLX-101) Cat No HY-19863





















































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor


































agonistreceptor


GR 113808Cat No HY-103152





GR 125743Cat No HY-121392
















61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor












61











of 397 nMKi




































antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor




















antagonist










an of 724 μMIC50















JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor






JNJ-18038683Cat No HY-19889


respectively




( =011 μM)IC50





















































LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor



























LY 344864Cat No HY-13788














LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor



LY310762Cat No HY-13527








LY334370Cat No HY-103107


with a of 16 nMKi














p s of 710 (5-HT ) 728 (5HT ) 756Kd 1A 1B

(5HT ) 699 (5HT ) 70 (5-HT ) 781C 1D 5A

(5-HT ) 874 (5-HT ) and 899 (5-HT ) and5B 6 7























binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor










binding assay










Houttfragrans







5-HT1A





















assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor












assays respectively





NEO 376 (SPI-376) Cat No HY-101583










nM























( =7 4 11 57 and 5H1 5HT2A2C 5HT3 5HT6 Ki










































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor







































respectively


































antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor
























antagonistreceptor





and 63 respectively













( =29 nM)Ki
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor
















PF-04995274Cat No HY-18137


agonist














93 respectively




















(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor













(pK =67)i





antagonist










PNU-142633Cat No HY-103131































receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor


















receptor











human D2 receptor













RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor



RG-12915Cat No HY-19110







respectively





















Ro 04-6790Cat No HY-14335








respectively)


























RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor

















RU 24969Cat No HY-16688


















SB 242084Cat No HY-13409






SB 243213Cat No HY-103112B
























SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor
















SB-200646Cat No HY-103129A







SB-200646ACat No HY-103129







SB-215505Cat No HY-18596


83 677 766 for 5-HT 5-HT 5-HT 2B 2A 2C






SB-269970Cat No HY-15370
















antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor





antagonist


SB-616234-ACat No HY-19477




SB228357Cat No HY-103154





































( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor






( =11 nM)Ki





( =11 nM)Ki













nM) receptors

















































TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor


























TG6-10-1Cat No HY-16978








or dopamine uptake







TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor



TIK-301 (PD-6735 LY-156735) Cat No HY-106136



respectively



























of 8 nMEC50












































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor









































WAY-181187 (SAX-187) Cat No HY-14340




































antagonistreceptor

























antagonistreceptor



5-HT Receptor · 2020. 7. 9. · 5-HT Receptor Antagonists, Agonists, Inhibitors & Modulators...

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Transcript of 5-HT Receptor · 2020. 7. 9. · 5-HT Receptor Antagonists, Agonists, Inhibitors & Modulators...