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Results for "

5-HT2A receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (168) Adrenergic Receptor (44) Apoptosis (15) Autophagy (10) COX (2) Cytochrome P450 (4) Dopamine Receptor (89) Drug Metabolite (6) GlyT (2) Histamine Receptor (16) Isotope-Labeled Compounds (23) mAChR (13) Mitophagy (5) P-glycoprotein (7) P2X Receptor (2) Parasite (1) Phosphatase (1) Reference Standards (30) Serotonin Transporter (5) Sigma Receptor (2) Sodium Channel (1) Transthyretin (TTR) (2) Wnt (1)
By Research Areas:	Cancer (28) Cardiovascular Disease (14) Endocrinology (14) Inflammation/Immunology (15) Metabolic Disease (9) Neurological Disease (158)

By Targets:

5-HT Receptor (168)

Adrenergic Receptor (44)

Apoptosis (15)

Autophagy (10)

COX (2)

Cytochrome P450 (4)

Dopamine Receptor (89)

Drug Metabolite (6)

GlyT (2)

Histamine Receptor (16)

Isotope-Labeled Compounds (23)

mAChR (13)

Mitophagy (5)

P-glycoprotein (7)

P2X Receptor (2)

Parasite (1)

Phosphatase (1)

Reference Standards (30)

Serotonin Transporter (5)

Sigma Receptor (2)

Sodium Channel (1)

Transthyretin (TTR) (2)

Wnt (1)

By Research Areas:

Cancer (28)

Cardiovascular Disease (14)

Endocrinology (14)

Inflammation/Immunology (15)

Metabolic Disease (9)

Neurological Disease (158)

179

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10560

Temanogrel APD791	5-HT Receptor	Neurological Disease
Temanogrel is a highly selective **5-HT_2A receptor** antagonist with a K_i of 4.9 nM.

HY-103115

Pruvanserin hydrochloride EMD 281014; LY 2422347 hydrochloride	5-HT Receptor	Neurological Disease
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin **5-HT_2A receptor** antagonist with IC₅₀ values of 0.35 nM and 1 nM for human and rat *5-HT_2A* receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .

HY-120820

LY320954	5-HT Receptor	Neurological Disease
LY320954 is a selective *5-HT2A* receptor antagonist, with a K_i of 96 nM. LY320954 potently inhibits Ca ²⁺ influx in the functional assay (EC₅₀ of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED₅₀ of 4.8 mg/kg .

HY-171235

5-HT2A antagonist 3	5-HT Receptor	Neurological Disease
5-HT2A antagonist 3 (Formula (III)) is a *5-HT2A* receptor antagonist and inverse agonist with a pIC₅₀ of 8.7 and a pK_i of 9. 5-HT2A antagonist 3 can be utilized in neurological reesearch .

HY-B2073A

Clocapramine dihydrochloride hydrate 3-Chlorocarpipramine dihydrochloride hydrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Clocapramine hydrochloride hydrate is an antagonist of the D₂ and **5-HT_2A receptors**.

HY-B2073

Clocapramine Clocarpramine; 3-Chlorocarpipramine	5-HT Receptor Dopamine Receptor	Neurological Disease
Clocapramine is an antagonist of the D₂, **5-HT_2A receptors**.

HY-10560A

Temanogrel hydrochloride APD791 hydrochloride	5-HT Receptor	Neurological Disease
Temanogrel hydrochloride is a highly selective **5-HT_2A receptor** antagonist with a K_i of 4.9 nM.

HY-123829

LY2624803	Histamine Receptor 5-HT Receptor	Inflammation/Immunology
LY2624803 is a 5-HT2A and histamine, H1 receptor antagonist .

HY-101619A

Abaperidone hydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
Abaperidone hydrochloride is a potent antagonist of **5-HT_2A receptor** and dopamine D₂ receptor with IC₅₀s of 6.2 and 17 nM.

HY-101619

Abaperidone	Dopamine Receptor 5-HT Receptor	Neurological Disease
Abaperidone is a potent antagonist of **5-HT_2A receptor** and dopamine D₂ receptor with IC₅₀s of 6.2 and 17 nM.

HY-118557

Iferanserin S-MPEC	5-HT Receptor	Inflammation/Immunology
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for **5-HT_2A receptor**. Iferanserin has the potential for internal hemorrhoid disease treatment .

HY-19417A

Wf-516	Serotonin Transporter 5-HT Receptor	Neurological Disease
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and *5-HT2A* receptors, with K_i of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.

HY-101690

QF0301B	Adrenergic Receptor	Cardiovascular Disease Endocrinology
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.

HY-101815

Lidanserin ZK-33839	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Lidanserin (ZK-33839) acts as a *5-HT_2A* and α₁-adrenergic receptor antagonist.

HY-19417

Wf-516 hydrochloride	Serotonin Transporter 5-HT Receptor	Neurological Disease
Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and *5-HT2A* receptors, with K_i of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.

HY-101250

Glemanserin MDL11939	Serotonin Transporter	Neurological Disease
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor *5-HT_2A* (K_i=2.89, 0.54 and 2.5 nM for rat 5-HT_2A, rabbit 5-HT_2A and human 5-HT_2A, respectively) .

HY-19733

Lumateperone tosylate ITI-007 tosylate	5-HT Receptor Dopamine Receptor	Neurological Disease Cancer
Lumateperone (ITI-007) tosylate is a *5-HT2A* receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .

HY-103104

Fananserin RP 62203	5-HT Receptor Dopamine Receptor	Neurological Disease
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT₂) receptor antagonist, with a K_i of 0.37 nM for the rat 5-HT_2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a K_i of 2.93 nM for the human dopamine D4 receptor .

HY-103136

R-96544	5-HT Receptor	Cardiovascular Disease
R-96544 is an orally active *5-HT_2A* receptor antagonist. R-96544 can inhibit platelet aggregation in vitro .

HY-172425

Deulumateperone	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Deulumateperone is a deuterium labeled Lumateperone (HY-17637). Lumateperone is the orally active **5-HT2A receptor** antagonist (K_i = 0.54 nM) and the modulator for dopamine receptor that exhibits antipsychotic and antineoplastic activities .

HY-10560R

Temanogrel (Standard) APD791 (Standard)	Reference Standards 5-HT Receptor	Neurological Disease
Temanogrel (Standard) is the analytical standard of Temanogrel. This product is intended for research and analytical applications. Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.

HY-A0019

Paliperidone 3 Publications Verification 9-Hydroxyrisperidone	Drug Metabolite Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .

HY-17637

Lumateperone ITI-007	Dopamine Receptor 5-HT Receptor	Neurological Disease Cancer
Lumateperone (ITI-007) is an orally active *5-HT2A* receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .

HY-164703

Lumateperone metabolite 1	Drug Metabolite Dopamine Receptor 5-HT Receptor	Neurological Disease
Lumateperone metabolite 1 (Formula T) is a metabolite of Lumateperone (HY-17637) . Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (K_i = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (K_i = 32 nM), and a dopamine D1 receptor modulator

HY-B0781S

Promethazine-d4 hydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Promethazine-d₄ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

HY-11018

Risperidone 5 Publications Verification R 64 766	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-15856

cis-(Z)-Flupentixol dihydrochloride cis-(Z)-Flupenthixol dihydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with K_i values of 0.38 nM and 7 nM for D2 receptor and *5-HT_2A*, respectively .

HY-101250R

Glemanserin (Standard) MDL11939 (Standard)	Reference Standards Serotonin Transporter	Neurological Disease
Glemanserin (Standard) is the analytical standard of Glemanserin. This product is intended for research and analytical applications. Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .

HY-101641

NRA-0160	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
NRA-0160 is a selective dopamine D4 receptor antagonist, with a K_i value of 0.48 nM and with negligible affinity for dopamine D2 receptor (K_i: >10000 nM), D3 receptor (K_i: 39 nM), rat **5-HT2A receptor (K_i: 180 nM) and rat α1 adrenoceptor (K_i**: 237 nM).

HY-11018A

Risperidone hydrochloride R 64 766 hydrochloride	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-B0781

Promethazine hydrochloride 1 Publications Verification	Histamine Receptor mAChR Adrenergic Receptor	Neurological Disease Endocrinology
Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .

HY-106246

Pruvanserin EMD 281014 free acid; LY 2422347	5-HT Receptor	Neurological Disease Metabolic Disease
Pruvanserin (EMD 281014 free acid) is a selective **5-HT2A receptor** antagonist. Pruvanserin alleviates tactile allodynia in diabetic rats. Pruvanserin can also be used for research of insomnia .

HY-103428

LE 300 2 Publications Verification	Dopamine Receptor 5-HT Receptor	Neurological Disease
LE 300 is a potent and selective dopamine D1-like receptor antagonist with K_is of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT_2A receptor with a pA2 of 8.32 in a rat tail artery assay .

HY-10792A

Eplivanserin (mixture) SR-46349 (mixture)	Serotonin Transporter 5-HT Receptor	Neurological Disease
Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a **5-HT_2A receptor** antagonist, extracted from patent WO 2005/002578 A1 .

HY-117118A

AC-90179	5-HT Receptor	Neurological Disease
AC-90179 is a selective *5-HT2A* receptor inverse agonist (K_i = 2.1 nM) and 5-HT2C antagonist, a potential antipsychotic compound .

HY-32329

Setiptiline Org-8282	5-HT Receptor Adrenergic Receptor	Neurological Disease
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

HY-A0019A

Paliperidone palmitate 9-Hydroxyrisperidone palmitate	Dopamine Receptor 5-HT Receptor	Neurological Disease
Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-11018B

Risperidone mesylate R 64 766 mesylate	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-10861

D3/5-HT receptor modulator-1	5-HT Receptor Dopamine Receptor	Neurological Disease
D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and **5-HT2A receptor** antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows K_i values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile .

HY-101630

Deramciclane EGIS-3886	5-HT Receptor	Neurological Disease
Deramciclane has a high affinity for *5-HT_2A* and 5-HT_2C 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.

HY-B1622

Cyproheptadine 3 Publications Verification	5-HT Receptor Apoptosis	Cardiovascular Disease Neurological Disease Cancer
Cyproheptadine is a potent and orally active **5-HT_2A receptor** antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders .

HY-B0366A

Cyproheptadine hydrochloride 3 Publications Verification Cyproheptadine HCl	5-HT Receptor	Cardiovascular Disease Neurological Disease Cancer
Cyproheptadine hydrochloride is a potent and orally active **5-HT_2A receptor** antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders .

HY-14148

Renzapride hydrochloride	5-HT Receptor	Neurological Disease
Renzapride hydrochloride is a benzamide that inhibits irritable bowel syndrome and has antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors. Renzapride hydrochloride also exhibits antagonistic activity at 5-HT(2B) receptors and has a certain affinity for 5-HT(2A) and 5-HT(2C) receptors .

HY-A0019S

Paliperidone-d4	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Paliperidone-d₄ is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .

HY-110232

Risperidone-d4 R 64 766-d₄	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone-d₄ is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

HY-32329A

Setiptiline maleate MO-8282	5-HT Receptor	Neurological Disease
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT_2A, 5-HT_2C, and/or 5-HT₃ subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-A0019R

Paliperidone (Standard) 9-Hydroxyrisperidone (Standard)	Drug Metabolite Reference Standards Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .

HY-B0781S1

Promethazine-d3 hydrochloride	Isotope-Labeled Compounds mAChR Adrenergic Receptor Histamine Receptor	Neurological Disease Endocrinology
Promethazine-d₃ (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .

HY-135194

Risperidone E-oxime	Drug Metabolite	Others
Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .

HY-123206

R-96544 free base	5-HT Receptor	Inflammation/Immunology
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits **5-HT2A receptor**-mediated contraction of guinea pig trachea .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-A0019

Paliperidone 3 Publications Verification 9-Hydroxyrisperidone	Structural Classification Natural Products Source classification Endogenous metabolite	Drug Metabolite Dopamine Receptor 5-HT Receptor Adrenergic Receptor
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .

HY-N1957

Gamma-Mangostin 2 Publications Verification γ-Mangostin	Structural Classification Xanthones Classification of Application Fields Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Metabolic Disease Plants Disease Research Fields	5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 ^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-N0049

Nuciferine 5 Publications Verification	Structural Classification Alkaloids Aporphine Alkaloids other families Source classification Plants Isoquinoline Alkaloids	Parasite 5-HT Receptor Dopamine Receptor
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-A0019R

Paliperidone (Standard) 9-Hydroxyrisperidone (Standard)	Structural Classification Natural Products Source classification Endogenous metabolite	Drug Metabolite Reference Standards Dopamine Receptor 5-HT Receptor Adrenergic Receptor
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .

HY-N1957R

Gamma-Mangostin (Standard) γ-Mangostin (Standard)	Structural Classification Xanthones Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Plants	Reference Standards 5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-N0049R

Nuciferine (Standard)	Structural Classification Alkaloids other families Source classification Plants	Reference Standards 5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Cat. No.	Product Name	Chemical Structure

HY-B0781S

Promethazine-d4 hydrochloride
Promethazine-d₄ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

HY-110232

Risperidone-d4
Risperidone-d₄ is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

HY-A0019S

Paliperidone-d4
Paliperidone-d₄ is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .

HY-B0781S1

Promethazine-d3 hydrochloride

Promethazine-d₃ (hydrochloride) is deuterium labeled Promethazine (hydrochloride). Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .

HY-17637S2

Lumateperone-d4

Lumateperone-d₄ (ITI-007-d₄) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .

HY-A0095S

Flibanserin-d4
Flibanserin-d₄ is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM) .

HY-32329S

Setiptiline-d3

Setiptiline-d₃ is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-19733S

Lumateperone-13C,d3 tosylate

Lumateperone- ¹³C,d₃ (ITI-007- ¹³C,d₃) tosylate is ¹³C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .

HY-11018S2

Risperidone-d6
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively .

HY-11018S1

Risperidone-d4-1
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-A0095S1

Flibanserin-d4-1

Flibanserin-d₄-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD) .

HY-A0077S2

Perphenazine-d6 fumarate

Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine . Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .

HY-14264S

Cyamemazine-d6
Cyamemazine-d₆ is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity .

HY-B0031S2

Quetiapine-d8 fumarate

Quetiapine-d₈ (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .

HY-B0031S3

Quetiapine-d8 hemifumarate

Quetiapine-d₈ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-15780S

Brexpiprazole-d8

Brexpiprazole-d₈ (OPC-34712-d₈) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM) ^.

HY-15780S1

Brexpiprazole-d8-1

Brexpiprazole-d₈-1 (OPC-34712-d₈-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM) .

HY-14539S3

Clozapine-d3

Clozapine-d₃ (HF 1854-d₃) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-B0731AS

Perospirone-d8

Perospirone-d₈ (SM-9018-d₈ (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT_2A receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of 5-HT_1A receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-B0031S5

Quetiapine-d4-1 fumarate

Quetiapine-d₄-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B0031S4

Quetiapine hemifumarate-d8

Quetiapine (hemifumarate)-d₈ is the deuterium labeled Quetiapine hemifumarate . Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-14544AS

Quetiapine-d4 hydrochloride

Quetiapine-d₄ (hydrochloride) (ICI204636-d₄ (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-14541S

Olanzapine-d3
Olanzapine-d₃ is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .

HY-14153S

Tegaserod-d11

Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-14541S2

Olanzapine-d8

Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic .

HY-B2169S2

Melperone-d4 hydrochloride

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-10564S

Sarpogrelate-d3 hydrochloride

Sarpogrelate-d₃ (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .

HY-10564S1

Sarpogrelate-d4 hydrochloride

Sarpogrelate-d₄ (MCI-9042-d₄) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT₂R antagonist, with pK_is of 8.52, 6.57, and 7.43 for 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT₁, 5-HT₃, 5-HT₄, α₁-, α₂- and β-adrenoreceptor, histamine H₁, H₂ and muscarinic M₃ receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .

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