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Results for "

human 5-HT2A receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (44) Adenylate Cyclase (1) Adrenergic Receptor (6) Apoptosis (4) DNA/RNA Synthesis (1) Dopamine Receptor (21) G protein-coupled Bile Acid Receptor 1 (1) Isotope-Labeled Compounds (8) Reactive Oxygen Species (ROS) (1) Reference Standards (5) Serotonin Transporter (5)
By Research Areas:	Cancer (5) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (4) Neurological Disease (41)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 Maximum Cited Publications 6 Publications Verification 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-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-14153

Tegaserod 4 Publications Verification	5-HT Receptor Apoptosis	Metabolic Disease Cancer
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-14153A

Tegaserod maleate 4 Publications Verification SDZ-HTF-919; HTF-919	5-HT Receptor Apoptosis	Neurological Disease Metabolic Disease Cancer
Tegaserod maleate (SDZ-HTF-919) is an orally active *serotonin receptor* 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B** receptor antagonist. Tegaserod maleate 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 maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-15543A

CP-809101 hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
CP-809101 hydrochloride is a potent and highly selective 5-HT_2C receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human 5HT_2C, 5HT_2B and *5HT_2A* receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .

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-116941

A-381393	Dopamine Receptor	Neurological Disease
A-381393 is a potent, selective, brain penetrate dopamine D₄ receptor antagonist, with K_is 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-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_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-153912

5-HT2A receptor agonist-3	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-3 ((S,S)-9b) is a **5-HT2A receptor agonist with a K_i** of 2.5 nM for human 5-HT2A receptor. 5-HT2A receptor agonist-3 shows 124-fold selectivity for *5-HT2A* over the structurally similar 5-HT2C receptor .

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-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-132225

SB 206553	5-HT Receptor	Inflammation/Immunology
SB 206553 is a 5-HT_2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT_2A), 7.7 nM (5-HT_2B) and 7.8 nM (5-HT_2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .

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-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_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-118796

4-Hydroxy MET 4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine	5-HT Receptor Serotonin Transporter	Neurological Disease
4-Hydroxy MET (4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine) is a synthetic tryptamine psychoactive substance. 4-Hydroxy MET is a partial 5-HT2A receptor agonist, a serotonin transporter inhibitor and weak norepinephrine transporter inhibitor. 4-Hydroxy MET affects emotional, motoric, and cognitive functions via serotonergic hallucinogenic activity .

HY-178760

TGF-8027	5-HT Receptor	Neurological Disease
TGF-8027 is a selective *5-HT_2A* agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC₅₀s of 3.3 nM, 160 nM and 7600 nM against human *5-HT_2A, 5-HT_2C* and 5-HT_2B and exhibits EC₅₀s against mouse 5-HT_2A and mouse 5-HT_2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT_2A receptor (such as depression) .

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-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-15401

WAY 163909	5-HT Receptor	Neurological Disease Metabolic Disease
WAY 163909 is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 exhibits an EC₅₀ of 8 nM and a K_i of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia .

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-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-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-B0031S2

Quetiapine-d8 fumarate	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
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-125641

AL-34662	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease
AL-34662 is a selective 5-HT2A receptoragonist (IC₅₀: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC₅₀:0.4 μM). AL-34662 is an ocular hypotensive agent .

HY-15543

CP-809101	5-HT Receptor	Neurological Disease
CP-809101 is a potent and highly selective 5-HT_2C receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human 5HT_2C, 5HT_2B and *5HT_2A* receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .

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-130351

25H-NBOMe hydrochloride	5-HT Receptor	Neurological Disease
25H-NBOMe hydrochloride is an agonist for the rat and human serotonin **5-HT2A receptors with K_i** values of 1.19 and 2.83 nM, 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-124367

25B-NBF hydrochloride	5-HT Receptor	Neurological Disease
25B-NBF hydrochloride is a highly potent agonist for the 5-HT2C receptor binds human 5-HT2A receptors and rat 5-HT2C receptors with pK_i values of 8.57 and 7.73, respectively .

HY-123480

EGIS-7625	5-HT Receptor	Neurological Disease
EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human K_i value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pK_i values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity .

HY-B0031S3

Quetiapine-d8 hemifumarate	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
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	Dopamine Receptor 5-HT Receptor	Neurological Disease
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	Dopamine Receptor 5-HT Receptor Isotope-Labeled Compounds	Neurological Disease
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-21995

BGC20-761	5-HT Receptor Dopamine Receptor	Neurological Disease
BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor K_i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent .

HY-14544AS

Quetiapine-d4 hydrochloride ICI204636-d4 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
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-14153S

Tegaserod-d11	5-HT Receptor Apoptosis Isotope-Labeled Compounds	Metabolic Disease Cancer
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-123480A

EGIS-7625 free base	5-HT Receptor	Neurological Disease
EGIS-7625 free base is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human K_i value of 1 nM. EGIS-7625 free base shows low affinity for 5-HT2A and 5-HT2C receptors. The pK_i values of EGIS-7625 free base for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 free base alleviates mCPP-induced hypoactivity .

HY-W609889

5-HT2A receptor agonist-14	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-14 (Compound I-23) is a tricyclic 5-HT2A receptor agonist with a pEC₅₀ value ≥ 6. 5-HT2A receptor agonist-14 can be used in research related to depression, anxiety, substance abuse and headache .

HY-183577

5-HT2A agonist 10	5-HT Receptor	Neurological Disease
5-HT2A agonist 10 is a 5-HT2A receptor agonist with an EC₅₀ of 9 nM. 5-HT2A agonist 10 is applicable to research related to central nervous system diseases .

HY-103104R

Fananserin (Standard) RP 62203 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Fananserin (Standard) is the analytical standard of Fananserin (HY-103104). This product is intended for research and analytical applications. 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-HT2A 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-121675A

2-Bromo-LSD D-Tartrate BOL-148 D-Tartrate; Bromolysergide D-Tartrate	5-HT Receptor G protein-coupled Bile Acid Receptor 1	Neurological Disease
2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT_2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC₅₀ of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a K_B of 0.18 nM for Gq dissociation) at the 5-HT_2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT_2A. 2-Bromo-LSD D-Tartrate lacks 5-HT_2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .

HY-W130288

1-(1-Naphthyl)piperazine	5-HT Receptor Adenylate Cyclase Apoptosis Reactive Oxygen Species (ROS)	Cancer
1-(1-Naphthyl)piperazine is a 5-HT receptor modulator that acts as both a *5-HT2A* receptor antagonist and 5-HT1A receptor agonist, and binds to human 5-HT6 receptor with a K_i of 120 nM. 1-(1-Naphthyl)piperazine partially inhibits forskolin-stimulated adenylate cyclase activity in calf substantia nigra. 1-(1-Naphthyl)piperazine inhibits UV-induced immunosuppression. 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis and increases ROS levels, leading to inhibit MNT-1 cell proliferation. 1-(1-Naphthyl)piperazine can be used for melanoma research .

HY-181613

5-HT2A&5-HT2C agonist-3	5-HT Receptor	Neurological Disease
5-HT2A&5-HT2C agonist-3 is an orally active and blood-brain barrier penetrant 5-HT2A and 5-HT2C agonist, with pEC₅₀ values of 7.79 and 7.10, respectively. 5-HT2A&5-HT2C agonist-3 elevates intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used in the research of neuropsychiatric disorders .

HY-182285A

FOXM1-IN-4 hydrochloride	5-HT Receptor DNA/RNA Synthesis	Cancer
FOXM1-IN-4 hydrochloride is a selective 5-HT₇ receptor inhibitor with a K_i of 92 nM. FOXM1-IN-4 hydrochloride blocks 5-HT₇ receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 hydrochloride acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G₂/M arrest, reduces G₀/G₁ population. FOXM1-IN-4 hydrochloride can be used for the research of triple-negative breast cancer .

Cat. No.	Product Name	Chemical Structure

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-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-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 .

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