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5-HT Receptor;5-hydroxytryptamine Receptor

5-HT receptors (Serotonin receptors) are a group of -coupled receptors (GPCRs) and -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 both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many , as well as many . The serotonin receptors influence various biological and neurological processes such as , , appetite, cognition, learning, memory, mood, , sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical , including many , , ,, gastroprokinetic agents, antimigraine agents, , and entactogens.

www.MedChemExpress.com 1 5-HT Receptor Inhibitors & Modulators

(4E)-SUN9221 (R,R)- Hydrochloride Cat. No.: HY-U00367 Cat. No.: HY-A0021C

Bioactivity: (4E)-SUN9221 is a potent antagonist of α1- Bioactivity: (R,R)-Palonosetron Hydrochloride is the active enantiomer of and 5-HT2 receptor, with antihypertensive and anti- Palonosetron. aggregation activities.

Purity: >98% Purity: 99.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 2 mg, 5 mg, 10 mg

(Z)-Thiothixene 5-HT1A modulator 1 Cat. No.: HY-108324 Cat. No.: HY-100290

Bioactivity: (Z)-Thiothixene is an antagonist of receptor Bioactivity: 5-HT1A modulator 1 displays very high affinities for the

extracted from patent US 20150141345 A1. 5HT1A, adrenergic α1 and D2 receptor with

IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

Purity: 99.14% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg

5-HT2 antagonist 1 5-HT2A antagonist 1 Cat. No.: HY-U00365 Cat. No.: HY-U00286

Bioactivity: 5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, Bioactivity: 5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from with weak α1 adrenoceptor blocking activity. patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

5-HT3 antagonist 1 5-HT3 antagonist 2 Cat. No.: HY-U00368 Cat. No.: HY-U00408

Bioactivity: 5-HT3 antagonist 1 is a potent and selective antagonist of Bioactivity: 5-HT3 antagonist 2 is a 5-HT3 . serotonin 3 (5-HT3) receptor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

5-HT3-In-1 5-HT4 antagonist 1 Cat. No.: HY-U00413 Cat. No.: HY-100170

Bioactivity: 5-HT3-In-1 is extracted from patent EP0748807A1, compound Bioactivity: 5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a example 8. It shows 5-HT3 inhibition activity. pKi of 9.6.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

5-HT6/7 antagonist 1 5-HT7 1 Cat. No.: HY-101622 Cat. No.: HY-109527

Bioactivity: 5-HT6/7 antagonist 1 is a multifunctional ligand that Bioactivity: 5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with antagonizes 5-HT6/7/2A and D2 receptors, without an IC50 of 222.93 nM, can be used for the 5-HT7 receptor interacting with M1 receptors and hERG channels. related disease, such as CNS disorders.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

5HT6-ligand-1 8-OH-DPAT Cat. No.: HY-U00126 (8-Hydroxy-DPAT) Cat. No.: HY-112061

Bioactivity: 5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of Bioactivity: 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC of 8.19 for 5-HT1A and a K of 466 nM for 5-HT7; 1.43 nM. 50 i

8-OH-DPAT weakly binds to 5-HT1B (pIC 50, 5.42), 5-HT (pIC

50 <5). Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Abaperidone Adoprazine Cat. No.: HY-101619 (SLV313) Cat. No.: HY-14782

Bioactivity: Abaperidone is a potent antagonist of 5-HT2Areceptor and Bioactivity: Adoprazine, a potential atypical bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. dopamine D2 receptor with IC50s of 6.2 and 17 nM.

Purity: >98% Purity: 98.13% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

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

Bioactivity: Agomelatine is a competitive antagonist of human and porcine Bioactivity: Agomelatine hydrochloride is a , which is serotonin (5-HT2C) receptors (pKi = 6.2 and 6.4, respectively) classified as a -dopamine disinhibitor (NDDI) as well as human 5-HT2B receptors (pKi = 6.6). IC50 value: 6.2 due to its antagonism of the 5-HT2C receptor. (pKi, 5-HT2c); 6.6 (pKi, 5-HT2b) Target: 5-HT2C Receptor; 5-HT2B receptor It is classified as a norepinephrine-dopamine… Purity: 99.88% Purity: 99.49% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) Cat. No.: HY-17038B (Alnitidan) Cat. No.: HY-101698

Bioactivity: Agomelatine (L(+)-Tartaric acid) is a antidepressant, which is Bioactivity: Alniditan is a potent 5-HT1B/1D receptors agonist, with classified as a norepinephrine-dopamine disinhibitor (NDDI) IC of 1.7 and 1.3 nM in HEK293 cells, and pK value of 8.96 due to its antagonism of the 5-HT2C receptor. 50 i and 9.40 for 5-HT 1B/1D receptors, respectively.

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

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Alosetron ((Z)-2-butenedioate) (GR 68755 (GR 68755; GR 68755X) Cat. No.: HY-70050A ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)) Cat. No.: HY-70050B

Bioactivity: Alosetron (GR 68755) is a Serotonin 5HT3-receptor antagonist Bioactivity: Alosetron (Z)-2-butenedioate (GR 68755 (Z)-2-butenedioate) is that is used in treatment of irritable bowel syndrome. IC50 a Serotonin 5HT3-receptor antagonist that is used in treatment Value: Target: 5-HT Receptor Alosetron has an antagonist of irritable bowel syndrome. IC50 Value: N/A Target: 5-HT action on the 5-HT3 receptors of the enteric of Receptor Alosetron has an antagonist action on the 5-HT3 the . While being a 5-HT3 antagonist… receptors of the enteric nervous system of the… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10 mg, 50 mg

Alosetron (Hydrochloride(1:X)) (GR 68755 Alosetron D3 Hydrochloride (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))) Cat. No.: HY-70050 (GR-68755C D3) Cat. No.: HY-70050CS

Bioactivity: Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is Bioactivity: Alosetron D3 Hydrochloride (GR-68755C D3) is deuterium labeled a Serotonin 5HT3-receptor antagonist that is used in treatment Alosetron, which is a serotonin 5HT3-receptor antagonist. of irritable bowel syndrome. IC50 Value: N/A Target: 5-HT3 Receptor Alosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 1 mg, 5 mg, 10 mg

Alosetron Hydrochloride (GR 68755C; GR 68755 (Hydrochloride); GR 68755X (Hydrochloride)) Cat. No.: HY-70050C ((RS)-Alprenolol; dl-Alprenolol) Cat. No.: HY-B1517

Bioactivity: Alosetron Hydrochloride (GR 68755 Hydrochloride) is a Bioactivity: Alprenolol is a non-selective as well as 5-HT1A Serotonin 5HT3-receptor antagonist that is used in treatment receptor antagonist. of irritable bowel syndrome. IC50 Value: Target: 5-HT Receptor Alosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract.… Purity: 99.72% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Alprenolol hydrochloride ((RS)-Alprenolol hydrochloride; Alverine citrate dl-Alprenolol hydrochloride) Cat. No.: HY-B1517A (NSC 35459) Cat. No.: HY-B0500

Bioactivity: Alprenolol (hydrochloride) is a non-selective beta blocker as Bioactivity: Alverine citrate is a 5-HT1A receptor antagonist, with an well as 5-HT1A receptor antagonist. IC50 of 101 nM.

Purity: 98.98% Purity: 98.71% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 g, 10 g

AM9405 Ansofaxine hydrochloride Cat. No.: HY-112707 (LY03005; LPM570065) Cat. No.: HY-U00096

Bioactivity: AM9405 is a novel peripherally active type 1 (CB1) Bioactivity: Ansofaxine hydrochloride (LY03005; LPM570065) is a triple and serotonin type 3 receptor agonist. AM9405 inhibits twitch inhibitor; inhibits serotonin, dopamine and

contraction of the ileum and the colon with IC50s of 45.71 and norepinephrine reuptake with IC50 values of 723, 491 and 763 0.076 nM, respectively. nM, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

AP521 AR-A 2 Cat. No.: HY-100166 (AR-A 000002) Cat. No.: HY-107018

Bioactivity: AP521 is an agonist of human 5-HT1A receptor with an IC50 Bioactivity: AR-A 2 is a selective 5-HT1B receptor antagonist, with high

of 94 nM. affinity to guinea pig cortex 5HT1B/1D and recombinant

guinea pig 5-HT1B receptors ( Ki=0.24 and 0.47 nM) and with

10-fold lower affinity to guinea pig 5-HT1D receptor ( Ki Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 250 mg, 500 mg

Aripiprazole D8 (OPC-14597) Cat. No.: HY-14546 (OPC-14597 D8) Cat. No.: HY-14546S

Bioactivity: Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial Bioactivity: Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled agonist with a Ki of 4.2 nM. Aripiprazole, which is a human 5-HT1A receptor with a Ki of 4.2 nM.

Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 100 mg, 200 mg, 500 mg, 1 g

Asenapine hydrochloride (Org 5222) Cat. No.: HY-10121 Cat. No.: HY-16567

Bioactivity: Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, Bioactivity: Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT 2B, , 5A, 6, 7) and Dopamine (D2, D3, D4) receptor receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 antagonist with K values of 0.03-4.0 nM for 5-HT and 1.3, nM. IC50 Value: 0.25-1.2 nM(Ki for adrenergic receptor); i 0.03-4.0 nM(Ki for 5-HT receptor) Target: 5-HT Receptor;… 0.42, 1.1 nM for , respectively. Purity: >98% Purity: 99.39% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Asenapine maleate AVN-492 (Org 5222 maleate) Cat. No.: HY-11100 Cat. No.: HY-101924

Bioactivity: Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) Bioactivity: AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R ( K =91 pM). and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, i respectively, and an antipsychotic.

Purity: 99.95% Purity: 99.49% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Azasetron hydrochloride (Y-25130 hydrochloride) Cat. No.: HY-B0068 (NLX-112; F13640) Cat. No.: HY-14785

Bioactivity: HCl is a selective 5-HT3 receptor antagonist with Bioactivity: Befiradol (NLX-112) is a selective 5-HT1A receptor agonist. IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer .

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 250 mg, 500 mg 10 mg, 50 mg, 100 mg, 200 mg

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Befiradol hydrochloride (NLX-112 (hydrochloride); F 13640 (hydrochloride)) Cat. No.: HY-14785A (MDL 72222) Cat. No.: HY-B1541

Bioactivity: Befiradol hydrochloride (NLX-112 hydrochloride) is a selective Bioactivity: Bemesetron (MDL 72222) is a selective 5-HT3 receptor 5-HT1A receptor agonist. [1] antagonist with an IC50 of 0.33 nM . Neuroprotective effect [2].

Purity: 99.22% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg

Blonanserin (AD-5423) Cat. No.: HY-13575 (OPC-34712) Cat. No.: HY-15780

Bioactivity: (AD-5423) is a D2/5-HT2 receptor antagonist, Bioactivity: Brexpiprazole is a partial agonist of human 5-HT1A and . Target: D2 receptor; 5-HT2 receptor dopamine receptor with Kis of 0.12 nM and 0.3 nM, Blonanserin(AD-5423) is a relatively new atypical respectively. Brexpiprazole is also a 5-HT2A receptor antipsychotic for the treatment of . Blonanserin antagonist with a K of 0.47 nM. belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and… i Purity: 99.77% Purity: 99.38% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

BRL 54443 BRL-15572 dihydrochloride Cat. No.: HY-13221 (BRL-15572) Cat. No.: HY-13200

Bioactivity: BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values Bioactivity: BRL-15572 2Hcl is a 5-HT1D receptor antagonist with pKi of are 8.7 and 8.9 respectively); displays > 30-fold 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B selectivity over other 5-HT and dopamine receptors. receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

Purity: 98.86% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 10 mg, 50 mg

Bromperidol hydrochloride (R-11333) Cat. No.: HY-B0901 Cat. No.: HY-B1115

Bioactivity: is a derivative, is a potent and Bioactivity: Buspirone hydrochloride is an psychotropic , is long-acting neuroleptic, used as an antipsychotic in the used to treat generalized anxiety disorder (GAD). treatment of schizophrenia.

Purity: 96.36% Purity: 99.64% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 100 mg

Cariprazine hydrochloride (RGH-188) Cat. No.: HY-14763 (RGH188 hydrochloride) Cat. No.: HY-14763A

Bioactivity: Cariprazine is a novel antipsychotic drug candidate that Bioactivity: Cariprazine hydrochloride is a novel antipsychotic drug

exhibits high affinity for the D3 ( Ki=0.085 nM) and D2 ( candidate that exhibits high affinity for the D3 ( Ki=0.085

Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A nM) and D2 ( Ki=0.49 nM) receptors, and moderate affinity

receptor ( Ki=2.6 nM). for the 5-HT1A receptor ( Ki=2.6 nM). Purity: 99.35% Purity: 99.89% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Chlorpromazine D6 hydrochloride hydrochloride Cat. No.: HY-B0407AS Cat. No.: HY-B0407A

Bioactivity: Chlorpromazine D6 hydrochloride is the deuterium labeled Bioactivity: Chlorpromazine Hydrochloride is an antagonist of the Chlorpromazine. Chlorpromazine is an inhibitor of dopamine dopamine D2, 5HT2A, potassium channel and sodium

receptor, 5-HT receptor, potassium channel, sodium channel. channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.

Purity: 99.0% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 1 mg, 5 mg, 10 mg

Cisapride (R 51619; (±)-Cisaprid) Cat. No.: HY-14149 (Clocarpramine; 3-Chlorocarpipramine) Cat. No.: HY-B2073

Bioactivity: (R 51619) is a nonselective 5-HT4 receptor agonist, Bioactivity: Clocapramine is an antagonist of the D2, 5-HT2A it is also a potent hERG potassium channel inhibitor. IC50 receptors. Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2] Target: 5-HT4 Receptor in vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50… Purity: 99.72% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg

Clocapramine hydrochloride hydrate N-oxide (3-Chlorocarpipramine hydrochloride hydrate) Cat. No.: HY-B2073A Cat. No.: HY-17366

Bioactivity: Clocapramine hydrochloride hydrate is an antagonist of the Bioactivity: Clozapine N-oxide (CNO) is a major metabolite of the

D2 and 5-HT2A receptors. anti-psychotic drug clozapine. Clozapine N-oxide is a agonist for the chemogenetic Designer Receptors Exclusively Activated by Designer Drug ( DREADD) system.

Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

CP-809101 CP-809101 hydrochloride Cat. No.: HY-15543 Cat. No.: HY-15543A

Bioactivity: CP-809101 is a potent and selective 5-HT2C receptor agonist Bioactivity: CP-809101 Hcl is a potent and selective 5-HT2C receptor with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A agonist with pEC50 of 9.96/7.19/6.81 for human receptors respectively. 5-HT2C/5-HT2B/5-HT2A receptors respectively.

Purity: >98% Purity: 99.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in Water, 10 mg, 50 mg

Cyclobenzaprine hydrochloride hydrochloride (MK130 hydrochloride) Cat. No.: HY-B0740 Cat. No.: HY-B0366A

Bioactivity: Hcl is a relaxant and a Bioactivity: Cyproheptadine is a receptor antagonist for 5-HT2 central nervous system (CNS) . receptor with IC50 of 0.6 nM.

Purity: 99.92% Purity: 98.96% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 50 mg, 100 mg, 500 mg, 1 g

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Cyproheptadine hydrochloride sesquihydrate Cat. No.: HY-B1165 (EGIS-3886) Cat. No.: HY-101630

Bioactivity: Cyproheptadine hydrochloride sesquihydrate is an Bioactivity: Deramciclane has a high affinity for 5-HT2A and 5-HT2C and is an antagonist of serotonin and histamine2. receptors; it acts as an antagonist at both receptor subtypes

and has inverse agonist properties at the 5-HT 2C receptors without direct stimulatory agonist. Purity: 99.20% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

Desipramine hydrochloride mesylate Cat. No.: HY-B1272 Cat. No.: HY-B0670A

Bioactivity: hydrochloride is an inhibitor of norepinephrine Bioactivity: Dihydroergotamine mesylate is an ergot alkaloid used to treat transporter ( NET), 5-HT transporter ( SERT) and migraines.

( DAT) with Kis of 4, 61 and 78,720 nM, respectively.

Purity: 99.68% Purity: 99.91% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 10 mg, 50 mg

Dolasetron Mesylate (MDL-73147) Cat. No.: HY-B0750 (MDL-73147EF) Cat. No.: HY-B0750A

Bioactivity: Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist Bioactivity: Dolasetron Mesylate (MDL-73147EF) is a serotonin 5-HT3 used to treat nausea and vomiting following chemotherapy. receptor antagonist used to treat nausea and vomiting following chemotherapy.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg, 10 mg

Dolasetron Mesylate hydrate hydrobromide (MDL-73147EF (hydrate)) Cat. No.: HY-B0750B (Eletriptan HBr) Cat. No.: HY-A0010

Bioactivity: Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist Bioactivity: Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor used to treat nausea and vomiting following chemotherapy. agonist with Ki of 0.92 nM and 3.14 nM, respectively. IC50 value: 0.82 nM/3.14 nM (5-HT1B/5-HT1D, Ki) [1] Target: 5-HT1B/5-HT1D in vitro: [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for… Purity: 99.0% Purity: 95.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg

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

Bioactivity: Eltoprazine(DU28853) is a serenic or antiaggressive agent Bioactivity: Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. an antagonist at the 5-HT2C receptor.

Purity: 95.0% Purity: 99.35% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 10 mg, 50 mg

8 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

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

Bioactivity: Eplivanserin is a potent, selective and orally available Bioactivity: Eplivanserin mixture is a selective serotonin reuptake 5-HT receptor antagonist, with an IC of 5.8 nM in rat 2 50 inhibitor and a 5-HT2A receptor antagonist, extracted from [1] cortical membrane, and a Kd of 1.14 nM. patent WO 2005/002578 A1 .

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Eptapirone Eucalyptol (F 11440) Cat. No.: HY-19946 (1,8-Cineole) Cat. No.: HY-N0066

Bioactivity: (F11440) is a potent, selective, high Bioactivity: Eucalyptol is an inhibitor of 5-HT3 receptor , potassium 5-HT1A receptor agonist with marked anxiolytic and channel, TNF-α and IL-1β. antidepressant potential.

Purity: 99.91% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 50 mg

F-15599 Ferulic acid sodium Cat. No.: HY-19863 (Sodium ferulate) Cat. No.: HY-N0060A

Bioactivity: F-15599 is a highly selective G-protein biased 5-HT1A Bioactivity: Ferulic acid (4-hydroxy-3-methoxycinnamic acid) is a phenolic compound present in several plants with claimed beneficial receptor agonist, with Ki of 3.4 nM. effects in prevention and treatment of disorders linked to oxidative stress and inflammation. IC50 value: Target: 5-HT Receptor In vitro: In the present study we have showed that… Purity: >98% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 1 g, 5 g

FK1052 hydrochloride Cat. No.: HY-101638 (BIMT-17; BIMT-17BS) Cat. No.: HY-A0095

Bioactivity: FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor Bioactivity: Flibanserin is a novel multifunctional serotonin agonist and dual antagonist. antagonist (MSAA) that improves sexual functioning in premenopausal women who suffer from reduced sexual interest and desire.

Purity: >98% Purity: 99.31% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Flopropione Cat. No.: HY-100562 (BRL 43694) Cat. No.: HY-B0071

Bioactivity: is a 5-HT1A receptor antagonist and also a Bioactivity: Granisetron (BRL 43694) is a serotonin 5-HT3 receptor catechol-o-methyltransferase ( COMT) inhibitor. antagonist used as an to treat nausea and vomiting following chemotherapy.

Purity: 98.37% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 50 mg, 100 mg 100 mg

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Granisetron Hydrochloride GSK163090 (BRL 43694A) Cat. No.: HY-B0071A Cat. No.: HY-14348

Bioactivity: Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor Bioactivity: GSK163090 is a potent, selective, and orally active 5-HT1A/B/D antagonist used as an antiemetic to treat nausea and vomiting receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for following chemotherapy. 5-HT1A/B/D, and dopamine D2/D3, respectively.

Purity: 99.69% Purity: 99.95% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Harmine (Telepathine) Cat. No.: HY-N0737A (Lu AE58054) Cat. No.: HY-14338

Bioactivity: Harmine is a natural dual-specificity Bioactivity: Idalopirdine (Lu AE58054) is a potent and selective 5-HT6 phosphorylation-regulated kinase ( (DYRK)) inhibitor with receptor antagonist with a Ki of 0.83 nM. anticancer and anti-inflammatory activities.

Purity: 99.78% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 500 mg

Idalopirdine Hydrochloride (Lu AE58054 (Hydrochloride)) Cat. No.: HY-14338A (HP 873) Cat. No.: HY-17410

Bioactivity: Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a Bioactivity: Iloperidone(HP 873) is a D2/5-HT2 receptor antagonist, which

potent and selective 5-HT6 receptor antagonist with a Ki of is an atypical antipsychotic for the treatment of 0.83 nM. schizophrenia symptoms.

Purity: 99.17% Purity: 99.93% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 10 mg, 50 mg, 100 mg

Iloperidone hydrochloride (HP 873 hydrochloride) Cat. No.: HY-17410A (SB-742457; GSK-742457; RVT-101) Cat. No.: HY-14339

Bioactivity: Iloperidone (hydrochloride) is a D(2)/5-HT(2) receptor Bioactivity: Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonistis, which is an atypical antipsychotic for the antagonist with pKi of 9.63; exhibits >100-fold selectivity treatment of schizophrenia symptoms. over other receptors.

Purity: >98% Purity: 98.92% Clinical Data: Launched Clinical Data: Phase 3 Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Irindalone Isocorynoxeine (Lu 21-​098) Cat. No.: HY-101632 (7-Isocorynoxeine) Cat. No.: HY-N0775

Bioactivity: Irindalone is a novel serotonin 5-HT2 antagonist. Bioactivity: Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A

receptor-mediated current response with an IC50 of 72.4 μM.

Purity: >98% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg

10 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

JNJ-18038683 Cat. No.: HY-19889 (R41468) Cat. No.: HY-10562

Bioactivity: JNJ-18038683 is a 5-Hydroxytryptamine Type 7 ( 5-HT7) Bioactivity: Ketanserin is a selective 5-HT receptor antagonist. Ketanserin also blocks hERG current ( IhERG) in a receptor antagonist, with pKis of 8.19, 8.20 for rat and human concentration-dependent manner ( IC =0.11 μM). 5-HT 7 in HEK293 cells, respectively. 50

Purity: >98% Purity: 98.86% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg

Ketanserin tartrate (R41468 tartrate) Cat. No.: HY-10562A (COL-144; LY573144) Cat. No.: HY-14861

Bioactivity: Ketanserin tartrate is a selective 5-HT receptor antagonist. Bioactivity: Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki Ketanserin tartrate also blocks hERG current ( IhERG) in a concentration-dependent manner ( IC =0.11 μM). of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, 50 respectively.

Purity: 99.97% Purity: >98% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 50 mg, 100 mg

Latrepirdine dihydrochloride dihydrochloride (Dimebolin dihydrochloride) Cat. No.: HY-14537 (E4424) Cat. No.: HY-101609

Bioactivity: dihydrochloride is a neuroactive compound with Bioactivity: Lesopitron dihydrochloride is a full and selective 5-HT1A antagonist activity at histaminergic, α-adrenergic, and receptor agonist with IC of 125 nM in rat hippocampal serotonergic receptors. Latrepirdine stimulates amyloid 50 precursor protein (APP) catabolism and amyloid-β ( Aβ) membranes. secretion. Purity: 99.75% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

Lidanserin Lintopride (ZK-33839) Cat. No.: HY-101815 Cat. No.: HY-U00121

Bioactivity: is a drug which acts as a combined 5-HT2A and Bioactivity: Lintopride is a 5HT4 antagonist with moderate 5HT3 antagonist properties. α1-adrenergic receptor antagonist.

Purity: 98.0% Purity: 96.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Loxapine succinate Cat. No.: HY-17390 Cat. No.: HY-17390A

Bioactivity: Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic Bioactivity: Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. agent.

Purity: 99.86% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg, 500 mg

www.MedChemExpress.com 11

LP-211 Tosylate Cat. No.: HY-111455 (ITI-007) Cat. No.: HY-19733

Bioactivity: LP-211 is a selective and −brain barrier penetrant Bioactivity: Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki =

5-HT7 receptor agonist, with a Ki of 0.58 nM, with high 0.54 nM), a partial agonist of presynaptic D2 receptors and an selectivity over 5-HT receptor (K , 188 nM) and D antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a 1A i 2 SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor (K , 142 nM). i receptor ) Target: 5-HT2A receptor Lumateperone also possesses… Purity: 99.66% Purity: 99.21% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

Lurasidone Hydrochloride (SM-13496) Cat. No.: HY-B0032A (SM-13496 (Hydrochloride)) Cat. No.: HY-B0032

Bioactivity: Lurasidone (SM-13496) is an antagonist of both dopamine Bioactivity: Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D and 5-HT with IC s of D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, 2 7 50 respectively. Lurasidone (SM-13496) is also a partial agonist 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist… of 5-HT1A receptor with an IC50 of 6.75 nM. Purity: 99.33% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

LY 344864 LY 344864 hydrochloride Cat. No.: HY-13788 Cat. No.: HY-13788B

Bioactivity: LY344864 is a selective receptor agonist with an affinity of 6 Bioactivity: LY 344864 hydrochloride is a selective 5-HT1F agonist with a nM (Ki) at the recently cloned 5-HT1F receptor. IC50 Value: 6 Ki of 6 nM. nM (Ki) [1] Target: 5-HT1F LY344864 possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1]. in vitro: he 5-HT1A, 5-HT1B and… Purity: 99.75% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg

LY 344864 racemate LY 344864 S-enantiomer Cat. No.: HY-13788C Cat. No.: HY-13788A

Bioactivity: LY 344864 racemate is a 5-HT1F receptor agonist extracted Bioactivity: LY 344864 S-enantiomer is the S-enantiomer of LY344864. from patent US 5708187 A. LY344864 is a 5-HT1F receptor agonist.

Purity: 98.88% Purity: 99.62% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 2 mg, 5 mg

LY310762 LY334370 Cat. No.: HY-13527 Cat. No.: HY-103107

Bioactivity: LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, Bioactivity: LY334370 is a selective 5-HT1F receptor agonist with a Ki of having a weaker affinity for 5-HT1B receptor. 1.6 nM.

Purity: 98.97% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

12 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Metergoline Methiothepin mesylate Cat. No.: HY-B1033 ( mesylate; Ro 8-6837 mesylate) Cat. No.: HY-107836

Bioactivity: is a of the chemical Bioactivity: Methiothepin mesylate is a potent and non-selective 5-HT2 class which acts as a ligand for various serotonin and receptor antagonist, with p K s of 7.10 (5-HT ), 7.28 dopamine receptors. d 1A (5HT 1B), 7.56 (5HT 1C), 6.99 (5HT 1D), 7.0 (5-HT 5A), 7.8

(5-HT 5B), 8.74 (5-HT 6), and 8.99 (5-HT 7), and p Kis… Purity: 99.74% Purity: 99.32% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 10 mg

MHP 133 Cat. No.: HY-101653 (Org3770; 6-Azamianserin) Cat. No.: HY-B0352

Bioactivity: MHP 133 is a drug with multiple CNS targets, and inhibits Bioactivity: Mirtazapine is a potent antidepressant.

acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg

Mosapride citrate (TAK-370; AS-4370) Cat. No.: HY-B0189 (TAK-370 citrate; AS-4370 citrate) Cat. No.: HY-B0189A

Bioactivity: Mosapride is a gastroprokinetic agent that acts as a selective Bioactivity: Mosapride citrate is a gastroprokinetic agent that acts as a 5HT4 agonist. selective 5HT4 agonist.

Purity: >98% Purity: 99.74% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Naftidrofuryl oxalate (Nafronyl oxalate salt) Cat. No.: HY-B1107 (PRX 00023) Cat. No.: HY-14848

Bioactivity: is a drug used in the management of peripheral Bioactivity: Naluzotan is a novel, potent, and selective amidosulfonamide

and cerebral vascular disorders as a vasodilator, enhance 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, cellular oxidative capacity, and may also be a 5-HT2 receptor used for the treatment of anxiety and depression; Also a weak antagonist. + hERG K , with IC 50 of 3800 nM. Purity: 97.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg

NAN-190 hydrobromide Cat. No.: HY-19818A (GR-85548A) Cat. No.: HY-B0197

Bioactivity: NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. Bioactivity: Naratriptan is a selective 5-HT1 receptor subtype agonist and NAN-190 is a selective antagonist of 5-HT1A. is a drug that is used for the treatment of migraine headaches.

Purity: 99.02% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 13

Naratriptan D3 Hydrochloride Naratriptan hydrochloride (GR-85548A D3) Cat. No.: HY-B0197AS (GR-85548A hydrochloride) Cat. No.: HY-B0197A

Bioactivity: Naratriptan D3 Hydrochloride is the deuterium labeled Bioactivity: Naratriptan hydrochloride is a selective 5-HT1 receptor Naratriptan, which is a selective 5-HT1 receptor subtype subtype agonist and is a triptan drug that is used for the agonist. treatment of migraine headaches.

Purity: >98% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Nefazodone hydrochloride (BMY-13754; MJ-13754-1) Cat. No.: HY-B1396 (APD125) Cat. No.: HY-10559

Bioactivity: hydrochloride is an antidepressant drug. Bioactivity: Nelotanserin is a potent 5-HT2A inverse agonist, a

moderately potent 5-HT2C partial inverse agonist and a weak

5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively. Purity: 99.71% Purity: 99.59% Clinical Data: Launched Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

NEO 376 Nexopamil racemate (SPI-376) Cat. No.: HY-101583 Cat. No.: HY-101727

Bioactivity: NEO 376 is a selective modulator of 5-HT1 receptor, GABA Bioactivity: Nexopamil racemate is the racemate of Nexopamil. Nexopamil is receptor and dopamine receptor, with anti-psychotic 2+ a combined Ca / 5-HT2 antagonist on thrombus formation in actively. vivo and on platelet aggregation in vitro.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

NPS ALX Compound 4a NRA-0160 Cat. No.: HY-103090 Cat. No.: HY-101641

Bioactivity: NPS ALX Compound 4a is a potent and selective Bioactivity: NRA-0160 is a selective dopamine D4 receptor antagonist, 5-hydroxytryptamine (5-HT ) receptor antagonist with an 6 6 with a Ki value of 0.48 nM and with negligible affinity for IC of 7.2 nM, which also has a great binding affinity with 50 dopamine D2 receptor ( Ki: >10000 nM), D3 receptor ( [1] K : 39 nM), rat 5-HT2A receptor ( K : 180 nM) and rat Ki of 0.2 nM . i i Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg

Nuciferine Cat. No.: HY-N0049 (R79598) Cat. No.: HY-101094

Bioactivity: is an antagonist at 5-HT2A ( IC50=478 nM), Bioactivity: Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A 5-HT2C ( IC50=131 nM), and 5-HT2B ( IC50=1 μM), an inverse agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 agonist at 5-HT7 ( IC50=150 nM), a partial agonist at D2 ( nM for 5-HT 2, a 1-adrenergic receptor, dopamine D 2 EC50=64 nM), D5 ( EC50=2.6 μM) and 5-HT6 ( EC50=… Purity: 99.66% Purity: 98.55% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg, 100 mg

14 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Olanzapine (LY170053) Cat. No.: HY-14541 (GR 38032; SN 307) Cat. No.: HY-B0002B

Bioactivity: (LY170053) is a high affinity for 5-HT2 serotonin Bioactivity: Ondansetron(GR 38032; SN 307) is a serotonin 5-HT3 receptor and D2 dopamine receptor antagonist. IC50 Value: Target: 5-HT antagonist used mainly as anantiemetic (to treat nausea and Receptor Olanzapine is a thienobenzodiazepine that blocks vomiting), often following chemotherapy. IC50 Value: Target: especially the serontonin (5-hydroxytryptamine [5-HT]) 5-HT2A 5- HT3 Receptor in vitro: 5-HT evoked transient inward and the dopamine D2 receptors (Ki values are 4 and 11 nM… currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were… Purity: 99.94% Purity: 98.55% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 500 mg

Ondansetron hydrochloride Ondansetron hydrochloride dihydrate (GR 38032 (hydrochloride (GR 38032 (hydrochloride); SN 307 (hydrochloride)) Cat. No.: HY-B0002 dihydrate); SN 307 (hydrochloride dihydrate)) Cat. No.: HY-B0002A

Bioactivity: Ondansetron hydrochloride (GR 38032 hydrochloride; SN 307 Bioactivity: Ondansetron hydrochloride dihydrate (GR 38032 hydrochloride hydrochloride) is a serotonin 5-HT3 receptor antagonist used dihydrate; SN 307 hydrochloride dihydrate) is a serotonin mainly as anantiemetic (to treat nausea and vomiting), often 5-HT3 receptor antagonist used mainly as anantiemetic (to following chemotherapy. Target: 5- HT Receptor IC50 Value: in treat nausea and vomiting), often following chemotherapy. vitro: 5-HT evoked transient inward currents (EC50 = 3.4… Target: 5- HT3 Receptor IC50 Value: in vitro: 5-HT evoked… Purity: >98% Purity: 99.56% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 50 mg, 100 mg, 1 g, 5 g

Palonosetron Palonosetron Hydrochloride Cat. No.: HY-A0018 Cat. No.: HY-A0021

Bioactivity: Palonosetron is a 5-HT3 antagonist used in the prevention and Bioactivity: Palonosetron Hcl is a 5-HT3 antagonist used in the prevention treatment of chemotherapy-induced nausea and vomiting (CINV). and treatment of chemotherapy-induced nausea and vomiting (CINV).

Purity: >98% Purity: 99.98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 100 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg

Pancopride (LAS 30451) Cat. No.: HY-19684 (SLV-308; DU-126891) Cat. No.: HY-14958

Bioactivity: Pancopride is a new potent and selective 5-HT3 receptor Bioactivity: Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 antagonist. receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8),… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Pardoprunox hydrochloride Peptide 401 (SLV-308 hydrochloride; DU-126891 hydrochloride) Cat. No.: HY-14958A Cat. No.: HY-12537

Bioactivity: Pardoprunox hydrochloride is a novel partial dopamine D2 and Bioactivity: Peptide 401, a potent mast cell degranulating factor from bee D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 venom, suppresses the increased vascular permeability due to (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and intradermal injection of various smooth muscle spasmogens ( 5-HT1A receptor (pKi = 8.5) full agonist. histamine, and 5-HT).

Purity: 98.89% Purity: 98.29% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 500u g, 1 mg, 5 mg

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Perphenazine D8 Dihydrochloride Cat. No.: HY-A0077 Cat. No.: HY-A0077AS

Bioactivity: Perphenazine is a drug, inhibits Bioactivity: Perphenazine D8 Dihydrochloride is the deuterium labeled

5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine Perphenazine, which is a typical antipsychotic drug(5-HT, receptor D2/D3, D2L receptor, and Histamine H1 receptor, Dopamine receptor ligand).

with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 … Purity: 99.90% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 1 g, 5 g

Phenylbiguanide (N-; PBG; 1-Phenylbiguanide) Cat. No.: HY-101331 (SB-207266) Cat. No.: HY-15574

Bioactivity: Phenylbiguanide is a 5-HT3 receptor selective agonist with Bioactivity: Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist. an EC50 of 3.0±0.1 μM.

Purity: 98.0% Purity: 98.85% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg

Piboserod hydrochloride (SB-207266 hydrochloride) Cat. No.: HY-15574A (ACP-103) Cat. No.: HY-14557

Bioactivity: Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor Bioactivity: Pimavanserin is a selective inverse agonist of the 5-HT2A antagonist. receptor with pIC50 and pKd of 8.73 and 9.3, respectively.

Purity: >98% Purity: 99.73% Clinical Data: Phase 2 Clinical Data: Launched Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Pimavanserin tartrate (ACP-103 tartrate) Cat. No.: HY-14557A (Pimetixene) Cat. No.: HY-B1101

Bioactivity: Pimavanserin tartrate (ACP-103) is a potent 5-HT 2A receptor Bioactivity: Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively. antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT 2C,

histamine H 1, dopamine D 2 and D 4.4 as well as muscari… Purity: 99.50% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Pimethixene maleate (Pimetixene maleate) Cat. No.: HY-B1101A (LB-46) Cat. No.: HY-B0982

Bioactivity: Pimethixene maleate is antihistamine and antiserotonergic Bioactivity: Pindolol (LB-46) is a nonselective β-blocker with partial compound, acts as an antimigraine agent. Pimethixene maleate beta-adrenergic receptor agonist activity, also functions as a

is a highly potent antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT1A receptor weak partial agonist / antagonist (Ki=33nM).

5-HT 2C, histamine H 1, dopamine D 2 and D 4.4 as well… Purity: >98% Purity: 99.84% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mg Size: 10mM x 1mL in DMSO, 100 mg

16 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pizotifen malate (BC-105; Pizotyline) Cat. No.: HY-B0115 (BC-105 (malate); Pizotyline (malate)) Cat. No.: HY-B0115A

Bioactivity: Pizotifen (BC-105) is a potent 5-HT2 receptor antagonist, Bioactivity: Pizotifen (malate) (BC-105 (malate)) is a potent 5-HT2

with a high affinity for 5-HT1C binding site. receptor antagonist, with a high affinity for 5-HT1C binding site.

Purity: 99.65% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg, 500 mg 100 mg, 200 mg, 500 mg

Prucalopride succinate Cat. No.: HY-14151 (R-108512) Cat. No.: HY-12694

Bioactivity: Prucalopride (R093877) is a drug acting as a selective, high Bioactivity: Prucalopride succinate is a selective, high affinity 5-HT4 affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b. >150-fold higher affinity for 5-HT4 receptors than for other receptors. IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi) Target: 5-HT4 receptor Prucalopride is a novel enterokinetic… Purity: 98.0% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg, 100 mg, 200 mg

PRX-08066 PRX933 hydrochloride Cat. No.: HY-15472 (GW876167 hydrochloride; BVT-933 hydrochloride) Cat. No.: HY-100171

Bioactivity: PRX-08066 is a selective 5-hydroxytryptamine receptor 2B Bioactivity: PRX933 hydrochloride is a 5-HT2c receptor agonist extracted (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective from patent WO 2014140631 A1. of pulmonary arteries.

Purity: 97.04% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg

Puerarin Pumosetrag Hydrochloride Cat. No.: HY-N0145 (MKC-733; DDP-733) Cat. No.: HY-19650

Bioactivity: Puerarin, an isoflavone extracted from Radix puerariae, is a Bioactivity: Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally 5-HT2C receptor antagonist. available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.

Purity: 98.14% Purity: 99.27% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Quetiapine D4 fumarate (ICI204636) Cat. No.: HY-14544 Cat. No.: HY-B0031S

Bioactivity: Quetiapine (ICI204636) is an atypical antipsychotic used in Bioactivity: Quetiapine D4 fumarate is the deuterium labeled Quetiapine, the treatment of schizophrenia, bipolar I mania, bipolar II which is an atypical antipsychotic. depression, bipolar I depression.

Purity: 99.83% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg, 10 mg

www.MedChemExpress.com 17

Quetiapine fumarate Hydrochloride Cat. No.: HY-B0031 (YM060) Cat. No.: HY-B0595

Bioactivity: Quetiapine fumarate is an atypical antipsychotic used in the Bioactivity: Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin treatment of schizophrenia, bipolar I mania, bipolar II 5-HT3 receptor antagonist for the treatment of nausea and depression, bipolar I depression. vomiting. Target: 5-HT3 Receptor Ramosetron hydrochloride selectively blocks serotonin receptors (5-HT3). Serotonin plays a vital role in vomiting, serotonin-induced bradycardic… Purity: 99.54 Purity: 99.85% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 10 mg, 50 mg

Revexepride RG-12915 Cat. No.: HY-U00373 Cat. No.: HY-19110

Bioactivity: Revexepride is a highly selective 5-HT4 receptor agonist, Bioactivity: RG-12915 is a selective 5-HT3 antagonist, with IC50 value of and a potential inducer of CYP3A4 enzyme, used for the 0.16 nM. treatment of gastroesophageal reflux disease.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

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

Bioactivity: Risperidone is a serotonin 5-HT2 receptor blocker, Bioactivity: Risperidone hydrochloride is a serotonin 5-HT2 receptor

P-Glycoprotein inhibitor and potent dopamine D2 receptor blocker and a potent dopamine D2 receptor antagonist,

antagonist, with Kis of 4.8, 5.9 nM for 5-HT 2A and dopamine with Kis of 0.16, 1.4 nM for 5-HT 2 and D 2 receptor,

D 2 receptor, respectively. respectively. Purity: 99.16% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Risperidone mesylate (R 64 766 mesylate) Cat. No.: HY-11018B (CYR-101; MIN-101; MT-210) Cat. No.: HY-19469

Bioactivity: Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 Bioactivity: Roluperidone (CYR-101) is a novel cyclic amide derivative that

receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 has high equipotent affinities for 5-HT2A and sigma-2 receptor antagonist(Ki= 1.4 nM). receptors ( Ki of 7.53 nM and 8.19 nM for 5-HT 2A and sigma-2, respectively). Purity: >98% Purity: 98.26% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Rotigotine Rotundine (N-0437; N-0923) Cat. No.: HY-75502 ((-)-; L-Tetrahydropalmatine) Cat. No.: HY-N0096

Bioactivity: is a full agonist of dopamine receptor, a Bioactivity: Rotundine is an antagonist of dopamine D1, D2 and D3

partial agonist of the 5-HT1A receptor, and an antagonist of receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, the α2B-adrenergic receptor, with Kis of 0.71nM, 4-15nM, and respectively. Rotundine is also an antagonist of 5-HT1A with 83nM for the dopamine D3 receptor and D2, D5, D4 receptors, an IC of 370 nM. and dopamine D1 receptor. 50 Purity: 99.98% Purity: 99.88% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 50 mg

18 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

RS 127445 RU 24969 (MT 500) Cat. No.: HY-15419 Cat. No.: HY-16688

Bioactivity: RS 127445 is a novel high affinity, selective 5-HT2B Bioactivity: RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors. receptor antagonist with pKi of 9.5.

Purity: 99.68% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

Rupatadine Fumarate (UR-12592) Cat. No.: HY-13511 (UR-12592 (Fumarate)) Cat. No.: HY-13511A

Bioactivity: Rupatadine (UR-12592) is a potent dual PAF/ with Bioactivity: Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet cerebellum membranes). IC50 value: Target: PAF/H1 antagonist membranes/guinea pig cerebellum membranes). IC50 value: in vitro: Rupatadine competitively inhibited histamine-induced Target: PAF/H1 antagonist in vitro: Rupatadine competitively guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without… inhibited histamine-induced guinea pig ileum contraction (pA2… Purity: >98% Purity: 99.34% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Sarpogrelate hydrochloride SB 242084 (MCI-9042) Cat. No.: HY-10564 Cat. No.: HY-13409

Bioactivity: hydrochloride (MCI-9042), a selective 5-HT2 Bioactivity: SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that antagonist, has been widely used as an anti-platelet agent for displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a receptors respectively. drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have the same affinity as… Purity: 98.39% Purity: 99.78% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

SB 242084 hydrochloride SB 258719 Cat. No.: HY-13409A Cat. No.: HY-U00443

Bioactivity: SB 242084 hydrochloride is a 5-HT2C receptor Bioactivity: SB 258719 is a selective 5-HT7 receptor antagonist with a antagonist(pKi=9.0) that displays 158- and 100-fold pK of 7.5. selectivity over 5-HT2A and 5-HT2B receptors respectively. i IC50 value: 9.0(pKi) [1] Target: 5-HT2C antagonist in vitro: SB 242084 had over 100-fold selectivity over a range of other… Purity: 98.58% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 50 mg

SB 271046 Hydrochloride SB-224289 hydrochloride (SB 271046A) Cat. No.: HY-14336A (SB-224289A) Cat. No.: HY-101105A

Bioactivity: SB271046 Hcl is a potent, selective and orally active 5-HT6 Bioactivity: SB-224289 hydrochloride is a selective 5-HT1B receptor receptor antagonist with pKi of 8.9. antagonist, with anxiolytic effect.

Purity: 99.06% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg

www.MedChemExpress.com 19

SB-269970 SB-269970 hydrochloride Cat. No.: HY-15370 (SB-269970A) Cat. No.: HY-15370A

Bioactivity: SB269970 is a 5-HT7 receptor antagonist with pKi of 8.3, Bioactivity: SB269970 hydrochloride is a hydrochloride salt form of exhibits >50-fold selectivity against other receptors. SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

Purity: >98% Purity: 99.41% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

SB-399885 hydrochloride SB-616234A Cat. No.: HY-103099 Cat. No.: HY-19477

Bioactivity: SB-399885 hydrochloride is a 5-HT6 receptor antagonist. Bioactivity: SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

Purity: 98.93% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Scopolamine Scopolamine hydrobromide ((-)-Scopolamine hydrobromide; (Hyoscine; Scopine (-)-tropate; Scopine tropate) Cat. No.: HY-N0296 Hyoscine hydrobromide; Scopine hydrobromide) Cat. No.: HY-N0296A

Bioactivity: Scopolamine is a high affinity (nM) muscarinic antagonist. Bioactivity: Scopolamine hydrobromide is a high affinity (nM) muscarinic

5-HT3 receptor-responses are reversibly inhibited by antagonist. 5-HT3 receptor-responses are reversibly

Scopolamine with an IC50 of 2.09 μM. inhibited by Scopolamine with an IC50 of 2.09 μM.

Purity: >98% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Serotonin hydrochloride (5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride) Cat. No.: HY-B1473 (Lu 23-174) Cat. No.: HY-14543

Bioactivity: Serotonin hydrochloride is a monoamine neurotransmitter in the Bioactivity: Sertindole, a neuroleptic, is one of the newer antipsychotic CNS and an endogenous 5-HT receptor agonist. Serotonin available. Target: Multi-target In vitro studies hydrochloride is also a catechol O-methyltransferase ( showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. COMT) inhibitor with a Ki of 44 μM. Sertindole offers an alternative treatment option for… Purity: 99.97% Purity: 96.14% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 10 mg, 50 mg

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

Bioactivity: Setiptiline(Org-8282) is a serotonin receptor antagonist. Bioactivity: Setiptiline is a serotonin receptor antagonist.

Purity: 96.00% Purity: 99.89% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

20 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Sulamserod T 82 (RS-100302) Cat. No.: HY-101668 Cat. No.: HY-U00028

Bioactivity: Sulamserod is a 5-HT4 receptor antagonist, with Bioactivity: T 82 is a potent 5-HT3 antagonist and acetylcholinesterase antiarrhythmic activities. (AChE) inhibitor, used for treatment of Alzheimer's Disease.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Talipexole dihydrochloride (B-HT 920 (dihydrochloride)) Cat. No.: HY-A0008 (SM-3997) Cat. No.: HY-14558

Bioactivity: dihydrochloride (B-HT 920 dihydrochloride) is a Bioactivity: Tandospirone(SM-3997) is a potent and selective 5-HT1A dopamine D2 receptor agonist, α2-adrenoceptor agonist and receptor partial agonist (Ki = 27 nM) that displays 5-HT3 receptor antagonist, which displays antiParkinsonian selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki activity. values ranging from 1300-41000 nM).

Purity: 99.99% Purity: 96.81% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg, 100 mg

Tandospirone citrate hydrobromide (SM-3997 citrate) Cat. No.: HY-B0061 (Lu AA 24530 hydrobromide) Cat. No.: HY-101755

Bioactivity: Tandospirone citrate is a potent and selective 5-HT1A receptor Bioactivity: Tedatioxetine hydrobromide acts as a triple

partial agonist (Ki = 27 nM) that displays selectivity over and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging antagonist. from 1300-41000 nM). IC50 Value: 27±5 nM(Ki) [1] Target: 5-HT1A in vitro: Tandospirone is most potent at the 5-HT1A… Purity: 98.87% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg

Tegaserod maleate Temanogrel (SDZ-HTF-919; HTF-919) Cat. No.: HY-14153A (APD791) Cat. No.: HY-10560

Bioactivity: maleate is a partial agonist of the 5-HT4 receptor; Bioactivity: Temanogrel is a highly selective 5-HT2A receptor antagonist stimulates the peristaltic reflex and accelerates with a K of 4.9 nM. gastrointestinal transit. i

Purity: 99.80% Purity: 98.14% Clinical Data: Launched Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 mg, 5 mg, 10 mg

Tertatolol TG6-10-1 ((±)​-​; Racemic Tertatolol; dl-​Tertatolol) Cat. No.: HY-U00356 Cat. No.: HY-16978

Bioactivity: Tertatolol is a potent antagonist of beta-adrenoceptor and Bioactivity: TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist 5-HT receptor, with unique renal vasodilatatory effects. activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors [1].

Purity: >98% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 21

Thioridazine hydrochloride Cat. No.: HY-B0965 Cat. No.: HY-90003

Bioactivity: is an antipsychotic drug, used in the treatment Bioactivity: Tianeptine is a selective facilitator of 5-HT uptake in vitro of schizophrenia and , shows D4 selectivity or and in vivo. IC50 Value: N/A Target: 5-HT Receptor Tianeptine serotonin antagonism. has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant, and… Purity: 99.93% Purity: 99.69% Clinical Data: Phase 4 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 50 mg

Tianeptine sodium salt hydrochloride Cat. No.: HY-90003A (AF-1161) Cat. No.: HY-B0478

Bioactivity: Tianeptine sodium salt is a selective facilitator of 5-HT Bioactivity: Trazodone (hydrochloride) (AF-1161) is an antidepressant uptake in vitro and in vivo. IC50 Value: Target: 5-HT Receptor belonging to the class of serotonin receptor antagonists and Tianeptine has no affinity for a wide range of receptors, reuptake inhibitors for treatment of anxiety disorders. including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant,… Purity: 99.88% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

Trimipramine maleate Cat. No.: HY-B1213 (SDZ-ICS-930 (free base)) Cat. No.: HY-B0072

Bioactivity: maleate is a 5-HT receptor antagonist, with pK is Bioactivity: Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 of 6.39, 8.10, 4.66 for 5-HT , 5-HT and 5-HT , receptor antagonist and α7-nicotinic receptor agonist with an 1C 2 1A IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± respectively. 0.9 nM [1] Target: 5-HT3 receptor in vitro: Tropisetron specifically inhibited both IL-2 gene transcription and IL-2… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg, 100 mg

Tropisetron Hydrochloride (SDZ-ICS-930) Cat. No.: HY-B0020 Cat. No.: HY-B0716

Bioactivity: Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 Bioactivity: Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor antagonist and α7-nicotinic receptor agonist with an receptor agonist. IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. IC50 value: 70.1 ± 0.9 nM Target: 5-HT3 receptor; α7-nicotinic receptor in vitro: Retinal ganglion cells(RGCs) pretreated with 100 nM… Purity: 99.64% Purity: 99.89% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 50 mg 10 mg, 50 mg, 100 mg

Urapidil hydrochloride hydrochloride Cat. No.: HY-B0354A (SCA 136) Cat. No.: HY-111200

Bioactivity: Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A Bioactivity: Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (

receptor agonist. 5-HT2C) receptor-selective agonist with an EC50 of 8 nM.

Purity: >98% Purity: 98.99% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

22 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Vilazodone D8 (EMD 68843; SB659746A) Cat. No.: HY-14262 Cat. No.: HY-14261S

Bioactivity: Vilazodone (EMD 68843; SB 659746A) is a combined serotonin Bioactivity: Vilazodone D8 is the a deuterium labeled vilazodone, which is specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial a combined serotonin specific reuptake inhibitor (SSRI) and agonist currently under clinical evaluation for the treatment 5-HT1A receptor partial agonist. of major depression.

Purity: 99.91% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 50 mg

Vilazodone Hydrochloride (EMD 68843 (Hydrochloride); SB659746A (Hydrochloride)) Cat. No.: HY-14261 (MDL100907; M 100907) Cat. No.: HY-14940

Bioactivity: Vilazodone Hydrochloride (EMD 68843 Hydrochloride; SB659746A Bioactivity: Volinanserin is a potent and selective antagonist of 5-HT2 Hydrochloride) is a (SER) inhibitor and receptor, with a Ki of 0.36 nM, and shows 300-fold 5-HT1A receptor partial agonist. selectivity for 5-HT 2 receptor over 5-HT 1c, alpha-1 and DA

D 2 receptors. Volinanserin has antipsychotic activity. Purity: 99.94% Purity: 99.71% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg

Vortioxetine hydrobromide (Lu AA 21004) Cat. No.: HY-15414 (Lu AA21004 hydrobromide) Cat. No.: HY-15414A

Bioactivity: Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, Bioactivity: Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, SERT with K values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 3.7 nM, 19 nM and 1.6 nM, respectively. i nM, respectively. Purity: 98.81% Purity: 99.54% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

WAY 163909 WAY-100635 Cat. No.: HY-15401 Cat. No.: HY-10349

Bioactivity: WAY 163909 is a potent and selective 5-HT(2C) receptor Bioactivity: WAY-100635 is a potent and selective 5-HT 1A Receptor agonist with a K of 10.5±1.1 nM. i antagonist with a pIC 50 of 8.87, an apparent pA 2 of 9.71.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

WAY-100635 Maleate WAY-100635 maleate salt Cat. No.: HY-10349A Cat. No.: HY-13105

Bioactivity: WAY-100635 Maleate is a potent and selective 5-HT 1A Receptor Bioactivity: WAY-100635 maleate salt is a potent and selective antagonist with a pIC of 8.87, an apparent pA of 9.71. 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ± 0.12 50 2 nM for 5-HT. IC50 Value: 0.95 nM Target: 5-HT Receptor in vitro: WAY 100635 has an IC50 of 1.35 nM and is > 100-fold selective for the 5-HT1A site relative to a range of other CNS… Purity: 98.0% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 23

Wf-516 Xanthotoxol Cat. No.: HY-19417A (8-Hydroxypsoralen) Cat. No.: HY-30152

Bioactivity: Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist Bioactivity: Xanthotoxol is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, antioxidant, 5-HT antagonistic, and neuroprotective effects. respectively, and has potent antidepressant activity.

Purity: >98% Purity: 99.15% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

YL0919 YM348 Cat. No.: HY-100769 Cat. No.: HY-100330

Bioactivity: YL0919, a novel antidepressant candidate with dual activity as Bioactivity: YM348 is a potent and orally active 5-HT2C receptor a 5-HT1A receptor agonist and a selective serotonin reuptake agonist, which shows a high affinity for cloned human 5-HT inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 2C receptor ( K : 0.89 nM). 5-HT into rat cerebral cortical synaptosomes and human i recombinant cells were 1.78±0.34 nM and 1.93±0.18 nM… Purity: 99.84% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Zatosetron maleate (LY 277359 maleate) Cat. No.: HY-U00234 (CP-88059) Cat. No.: HY-14542

Bioactivity: maleate is a potent and selective 5HT3 receptor Bioactivity: Ziprasidone(CP88059) is a combined 5-HT (serotonin) and antagonist. dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.

Purity: >98% Purity: 98.69% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

Ziprasidone D8 Ziprasidone hydrochloride (CP-88059 D8) Cat. No.: HY-14542S (CP-88059 hydrochloride) Cat. No.: HY-14542A

Bioactivity: Ziprasidone D8 is deuterium labeled Ziprasidone, which is a Bioactivity: Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) combined 5-HT (serotonin) and dopamine receptor antagonist and dopamine receptor antagonist which exhibits potent effects which exhibits potent effects of antipsychotic activity. of antipsychotic activity.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mg, 50 mg

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

Bioactivity: Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. Target: 5-HT receptor; Dopamine receptor Ziprasidone hydrochloride monohydrate is the salt… Purity: 99.83% Clinical Data: Launched Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]