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human dopamine receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Dopamine Receptor (100) Dopamine Transporter (3) 5-HT Receptor (39) Adenosine Receptor (1) Adrenergic Receptor (10) Apoptosis (2) Autophagy (2) Bacterial (6) Calcium Channel (2) Drug Derivative (1) Drug Intermediate (1) Drug Metabolite (6) ERK (4) Fluorescent Dye (1) Histamine Receptor (7) iGluR (1) Influenza Virus (1) Isotope-Labeled Compounds (12) mAChR (12) Monoamine Transporter (7) mTOR (2) nAChR (1) Neurokinin Receptor (1) p38 MAPK (2) PDGFR (2) Phosphodiesterase (PDE) (1) Phospholipase (2) Potassium Channel (2) Reactive Oxygen Species (ROS) (1) Reference Standards (17) Serotonin Transporter (4) Sodium Channel (1) Trk Receptor (1) UGT (1)
By Research Areas:	Cancer (15) Cardiovascular Disease (3) Infection (5) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (107)

By Targets:

Dopamine Receptor (100)

Dopamine Transporter (3)

5-HT Receptor (39)

Adenosine Receptor (1)

Adrenergic Receptor (10)

Apoptosis (2)

Autophagy (2)

Bacterial (6)

Calcium Channel (2)

Drug Derivative (1)

Drug Intermediate (1)

Drug Metabolite (6)

ERK (4)

Fluorescent Dye (1)

Histamine Receptor (7)

iGluR (1)

Influenza Virus (1)

Isotope-Labeled Compounds (12)

mAChR (12)

Monoamine Transporter (7)

mTOR (2)

nAChR (1)

Neurokinin Receptor (1)

p38 MAPK (2)

PDGFR (2)

Phosphodiesterase (PDE) (1)

Phospholipase (2)

Potassium Channel (2)

Reactive Oxygen Species (ROS) (1)

Reference Standards (17)

Serotonin Transporter (4)

Sodium Channel (1)

Trk Receptor (1)

UGT (1)

By Research Areas:

Cancer (15)

Cardiovascular Disease (3)

Infection (5)

Inflammation/Immunology (1)

Metabolic Disease (1)

Neurological Disease (107)

116

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Dopamine Receptor Dopamine β-hydroxylase Dopamine Transporter

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17366

Clozapine N-oxide Maximum Cited Publications 145 Publications Verification	Drug Metabolite mAChR Dopamine Receptor	Neurological Disease
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the *DREADD receptor* hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine** antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist .

HY-17366A

Clozapine N-oxide dihydrochloride Maximum Cited Publications 145 Publications Verification	mAChR Dopamine Receptor Drug Metabolite	Neurological Disease
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the *DREADD receptor* hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride cannot cross the blood-brain barrier . Clozapine is a potent dopamine** antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist .

HY-19545A

SCH-23390 hydrochloride 30+ Cited Publications R-(+)-SCH-23390 hydrochloride	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective **dopamine D₁-like receptor antagonist with K_i*s of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy *human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂** and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM .

HY-14544

Quetiapine 3 Publications Verification ICI204636	5-HT Receptor Dopamine Receptor	Neurological Disease
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-15780

Brexpiprazole 5+ Cited Publications OPC-34712	5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
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 α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM) .

HY-B0590

Tetrabenazine 1 Publications Verification Ro 1-9569	Monoamine Transporter Dopamine Receptor	Neurological Disease
Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks **dopamine D2 receptors*, and increases dopamine* turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-B0520A

Benztropine mesylate 5 Publications Verification Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate	Dopamine Receptor mAChR Histamine Receptor	Infection Neurological Disease Metabolic Disease Cancer
Benztropine mesylate (Benzatropine mesylate) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a **human D₂ dopamine receptor** allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-B0590S

Tetrabenazine-d6 Ro 1-9569-d₆	Monoamine Transporter	Neurological Disease
Tetrabenazine-d₆ (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks **dopamine D2 receptors*, and increases dopamine* turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-B0031

Quetiapine hemifumarate 3 Publications Verification	5-HT Receptor Dopamine Receptor	Neurological Disease
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-128770

LY3154207 2 Publications Verification	Dopamine Receptor	Neurological Disease
LY3154207 is a potent, subtype selective, and orally available **human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC₅₀**=3 nM) .

HY-100656

Desmethyl cariprazine	Dopamine Receptor 5-HT Receptor	Neurological Disease
Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC₅₀ of 8.90 at human D2 receptors, a pEC₅₀ of 8.09 at D3 receptors, and a pEC₅₀ of 6.28 at 5-HT_1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT_1A receptors, and suppresses serotonin-induced Ca ²⁺ release at 5-HT_2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

HY-101348

L-741626 2 Publications Verification	Dopamine Receptor	Neurological Disease
L-741626 is a selective D2 dopamine receptor antagonist, with the K_i values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .

HY-14545

Amisulpride 2 Publications Verification (Rac)-Aramisulpride; (Rac)-Esamisulpride; DAN 2163	Dopamine Receptor 5-HT Receptor	Neurological Disease
Amisulpride ((Rac)-Aramisulpride) is a racemic (50:50) mixture of the R-Amisulpride (HY-109167) and S-Amisulpride (HY-126068). Amisulpride is a dopamine D₂/D₃ receptor antagonist with K_i values of 2.8 and 3.2 nM for human dopamine b>D₂ and b>D₃, respectively. Amisulpride is a 5-HT₇ receptor antagonist with a K_i of 44 nM. Amisulpride can be used in psychiatric research .

HY-B0590A

Tetrabenazine Racemate Ro 1-9569 Racemate	Monoamine Transporter Dopamine Receptor	Neurological Disease
Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks **dopamine D2 receptors*, and increases dopamine* turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-A0125A

Alizapride hydrochloride	Dopamine Receptor	Neurological Disease Cancer
Alizapride is a potent antiemetic, acting as a **dopamine receptor** antagonist. Alizapride also used in human digestive disorders .

HY-101382

GR 103691 2 Publications Verification	Dopamine Receptor	Neurological Disease
GR 103691 is a potent, selective **dopamine D₃ receptor antagonist with a K_i** value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D₃ over hD₄ and hD₁ sites .

HY-110000

(+)-PD 128907 hydrochloride	Dopamine Receptor	Neurological Disease
(+)-PD 128907 hydrochloride is a selective dopamine D₂/D₃ receptor agonist, with K_is of 1.7, 0.84 nM for human and rat D₃ receptors, 179, 770 n M for human and rat D₃ receptors, respectively.

HY-119093

Halopemide 1 Publications Verification	Phospholipase Dopamine Receptor	Neurological Disease Cancer
Halopemide is a potent phospholipase D (PLD) inhibitor, with IC₅₀s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a **dopamine receptors** antagonist, and acts a psychotropic agent .

HY-B0520

Benztropine 5 Publications Verification Benzatropine; Benzotropine	Dopamine Receptor mAChR Histamine Receptor	Cancer
Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a **human D₂ dopamine receptor** allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-100820

Sarizotan 1 Publications Verification EMD 128130	5-HT Receptor Dopamine Receptor	Neurological Disease
Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and **dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀** values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively .

HY-10847B

SB-277011 hydrochloride 1 Publications Verification SB-277011A hydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor (D₃R) antagonist with K_i values of 10.7 nM and 11.2 nM at rodent and human D₃R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pK_is of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT_1B, and 5-HT_1D receptors, respectively .

HY-N2411

Geissoschizine methyl ether 1 Publications Verification	5-HT Receptor	Neurological Disease
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ ³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .

HY-115553

DETQ	Dopamine Receptor	Neurological Disease
DETQ is a selective, allosteric and orally active **dopamine D1 receptor (Dopamine Receptor*) potentiator. In HEK293 cells expressing the human* D1 receptor, DETQ increases cAMP with an EC₅₀ of 5.8 nM and a K_b of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor .

HY-14545A

Amisulpride hydrochloride 2 Publications Verification (Rac)-Aramisulpride hydrochloride; (Rac)-Esamisulpride hydrochloride; (Rac)-DAN 2163 hydrochloride	Dopamine Receptor	Neurological Disease
Amisulpride hydrochloride is a dopamine D₂/D₃ receptor antagonist with K_is of 2.8 and 3.2 nM for human dopamine D₂ and D₃, respectively.

HY-148867

UCM-1306	Dopamine Receptor	Neurological Disease
UCM-1306 is a potent and orally active human **dopamine D1 receptor** allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD) .

HY-14545S

Amisulpride-d5 (Rac)-Aramisulpride-d₅; (Rac)-Esamisulpride-d₅; DAN 2163-d₅	Dopamine Receptor	Neurological Disease Cancer
Amisulpride-d₅ is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with K_is of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .

HY-116941

A-381393	Dopamine Receptor	Neurological Disease
A-381393 is a potent, selective, brain penetrate **dopamine D₄ receptor antagonist, with K_i*s of 1.5, 1.9 and 1.6 nM for human* dopamine D_4.4, D_4.2, and D_4.7 receptor, respectively, >2700-fold selectivity over D₁, D₂, D₃ and D₅ dopamine receptors. A-381393 shows moderate affinity for 5-HT_2A (K_i, 370 nM) .

HY-14325

L-745870 3 Publications Verification	Dopamine Receptor	Neurological Disease
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors .

HY-14325B

L-745870 hydrochloride 3 Publications Verification	Dopamine Receptor	Neurological Disease
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors .

HY-15780S1

Brexpiprazole-d8-1 OPC-34712-d₈-1	Isotope-Labeled Compounds Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
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_i*s 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-W722043

MFZ 2-13 O-456	Drug Intermediate Dopamine Receptor	Neurological Disease
MFZ 2-13 (O-456) is an N-demethylated intermediate and N-nor-analogue of MFD 2-12. MFZ 2-13 inhibits *dopamine* uptake through the human **dopamine receptor with an IC₅₀** of 1.4 nM .

HY-103409

ABT-724 trihydrochloride	Dopamine Receptor	Neurological Disease
ABT-724 trihydrochloride is a potent and highly selective **dopamine D₄ receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D₄ receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D₄ (EC₅₀** of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM), and has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .

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_i*s 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-14544R

Quetiapine (Standard) ICI204636 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine (Standard) is the analytical standard of Quetiapine. This product is intended for research and analytical applications. 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-B0031R

Quetiapine hemifumarate (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. 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-17366R

Clozapine N-oxide (Standard)	Reference Standards mAChR Dopamine Receptor Drug Metabolite	Neurological Disease
Clozapine N-oxide (Standard) is the analytical standard of Clozapine N-oxide. This product is intended for research and analytical applications. Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide cannot cross the blood-brain barrier[1][2][3][4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].

HY-133152

Brexpiprazole S-oxide DM-3411	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide (DM-3411) 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-HT_1A and **dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT_2A** receptor antagonist with a K_i of 0.47 nM .

HY-15780R

Brexpiprazole (Standard) OPC-34712 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. 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 α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM) .

HY-135096

Amitriptyline-d3 hydrochloride	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease
Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .

HY-15780S

Brexpiprazole-d8 OPC-34712-d₈	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
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_i*s 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-14330

ABT-724	Dopamine Receptor	Neurological Disease
ABT-724, a chemical probe, is a potent and highly selective **dopamine D₄ receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D₄ receptor. ABT-724 is a potent partial agonist at the rat D₄ (EC₅₀** of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM). ABT-724 has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .

HY-15780A

Brexpiprazole hydrochloride OPC-34712 hydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A** receptor antagonist with a K_i of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM) .

HY-177122

Raxlaprazine etomoxil	Dopamine Receptor	Neurological Disease
Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (K_i) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC₅₀) of 3.72 nM in functional activity experiments .

HY-133152S

Brexpiprazole S-oxide-d8 DM-3411 d₈	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide-d₈ (DM-3411 D₈) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). 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-103405A

NGD 94-1 dimaleate	Dopamine Receptor	Neurological Disease
NGD 94-1 (dimaleate) is a potent and selective **dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (K_i** = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research ^[1][2].

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-A0125

Alizapride	Dopamine Receptor	Neurological Disease
Alizapride is a potent antiemetic, acting as a **dopamine receptor** antagonist. Alizapride also used in human digestive disorders .

HY-14325R

L-745870 (Standard)	Dopamine Receptor	Neurological Disease
L-745870 (Standard) is the analytical standard of L-745870. This product is intended for research and analytical applications. L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .

HY-19483

ABT-670	Dopamine Receptor	Neurological Disease
ABT-670 is a selective, oral bioavailable agonist of **dopamine D₄ receptor, with EC₅₀** of 89 nM, 160 nM, and 93 nM for human D₄, ferret D₄, and rat D₄, respectively.

HY-109150

Mesdopetam IRL790	Dopamine Receptor	Neurological Disease
Mesdopetam (IRL790) is a dopamine D3 receptor antagonist (K_i=90 nM; IC₅₀=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease .

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library

3,389 compounds

GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.

MCE provides a unique collection of 3,389 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2411

Geissoschizine methyl ether 1 Publications Verification	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Structural Classification Rubiaceae Plants Indole Alkaloids Source Classification	5-HT Receptor
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ ³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .

HY-N3945R

Glaucine (Standard) O,O-Dimethylisoboldine (Standard); S-(+)-Glaucine (Standard); NSC 34396 (Standard)	Alkaloids Structural Classification other families Plants Isoquinoline Alkaloids Glaucium flavum Papaveraceae Source Classification	Reference Standards Phosphodiesterase (PDE) Calcium Channel Adrenergic Receptor Dopamine Receptor Influenza Virus
Glaucine (Standard) is the analytical standard of Glaucine. This product is intended for research and analytical applications. Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 μM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities .

HY-N18249

Rehmaglupentasaccharide A	Structural Classification Rehmannia glutinosa (Gaertn.) Libosch. ex Fisch. & C. A. Mey. Orobanchaceae Plants Saccharides Source Classification	Bacterial
Rehmaglupentasaccharide A is a pentasaccharide found in air-dried roots of Rehmannia glutinosa. Rehmaglupentasaccharide A promotes proliferation of Lactobacillus reuteri .

HY-N18271

Rehmaglupentasaccharide B	Structural Classification Natural Products Rehmannia glutinosa (Gaertn.) Libosch. ex Fisch. & C. A. Mey. Orobanchaceae Plants Source Classification	Bacterial
Rehmaglupentasaccharide B is a pentasaccharide which can be found in the roots of dried Rehmannia glutinosa. Rehmaglupentasaccharide B promotes the proliferation of Lactobacillus reuteri .

Cat. No.	Product Name	Chemical Structure

HY-B0590S

Tetrabenazine-d6

Tetrabenazine-d₆ (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-14545S

Amisulpride-d5
Amisulpride-d₅ is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with K_is of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .

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-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-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ (DM-3411 D₈) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). 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-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-B0590S3

Tetrabenazine-d7

Tetrabenazine-d₇ (TBZ-d₇-d₇) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-14545S1

Amisulpride-d5 N-Oxide
Amisulpride-d₅ N-Oxide is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with K_is of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .

HY-B0520AS1

Benztropine-d3 mesylate

Benztropine-d₃ (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-B0520AS

Benztropine-13C,d3 mesylate

Benztropine- ¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

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-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-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-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-W748582

Clozapine N-oxide-d8

Clozapine N-oxide-d₈ is the deuterium labeled Clozapine N-oxide (HY-17366). Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist .

HY-100656AS

Desmethyl cariprazine-d8

Desmethyl cariprazine-d₈ is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC₅₀ of 8.90 at human D2 receptors, a pEC₅₀ of 8.09 at D3 receptors, and a pEC₅₀ of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca ²⁺ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

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