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5-HT2 Receptor Agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (233) Adenylate Cyclase (1) Adrenergic Receptor (19) Androgen Receptor (1) Apoptosis (5) Autophagy (5) Bacterial (2) Calcium Channel (1) Dopamine Receptor (66) Dopamine Transporter (2) Drug Derivative (1) Drug Metabolite (5) Endogenous Metabolite (7) G protein-coupled Bile Acid Receptor 1 (2) G Protein-coupled Receptor Kinase (GRK) (1) GABA Receptor (2) HCN Channel (2) Hedgehog (1) Histamine Receptor (2) Interleukin Related (1) Isotope-Labeled Compounds (24) Ligands for E3 Ligase (1) mAChR (8) Melatonin Receptor (11) Monoamine Oxidase (1) Monoamine Transporter (1) P2X Receptor (2) Parasite (3) Phosphatase (1) Potassium Channel (2) Reactive Oxygen Species (ROS) (1) Reference Standards (34) Serotonin Transporter (5) Sigma Receptor (1) Smo (2) Sodium Channel (3) STAT (1) TNF Receptor (1) TRP Channel (2)
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244

Inhibitors & Agonists

Biochemical Assay Reagents

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Isotope-Labeled Compounds

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19545A

SCH-23390 hydrochloride Maximum Cited Publications 31 Publications Verification 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_is 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-14546

Aripiprazole 10+ Cited Publications OPC-14597	5-HT Receptor Dopamine Receptor	Infection Neurological Disease Inflammation/Immunology
Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at *5-HT2B* and *5-HT2A* receptors and displays partial agonist actions at 5-HT1A, *5-HT2C, D3, and D4 receptors*. Aripiprazole can be used for the research of schizophrenia and COVID19 .

HY-103124

DOI hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
DOI hydrochloride is a serotonin **5-HT_2A/_2C receptor** agonist with K_i values of 0.7 nM, 2.4 nM and 20 nM for h5-HT_2A, h5-HT_2C and h5-HT_2B receptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice .

HY-14557

Pimavanserin 10+ Cited Publications ACP-103	5-HT Receptor	Neurological Disease
Pimavanserin is a selective, brain-penetrant, inverse agonist of the *5-HT2A* receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-156601

Bexicaserin LP352	5-HT Receptor	Neurological Disease
Bexicaserin (LP352) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related disorders (such as epilepsy) .

HY-172420

Bretisilocin GM-2505	5-HT Receptor	Neurological Disease
Bretisilocin (GM-2505) is the agonist for **5-HT_2A receptor** and a serotonin releaser. Bretisilocin exhibits antidepressant activity and can be used in the study of depression .

HY-14546A

Aripiprazole monohydrate 10+ Cited Publications OPC-14597 monohydrate	5-HT Receptor Dopamine Receptor	Infection Neurological Disease Inflammation/Immunology
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at *5-HT2B* and *5-HT2A* receptors and displays partial agonist actions at 5-HT1A, *5-HT2C, D3, and D4 receptors*. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19 .

HY-12714

TDHL Tergurid; Terguride; trans-Dihydrolisuride	Dopamine Receptor 5-HT Receptor	Neurological Disease
TDHL (Tergurid) is a dopamine receptor agonist with a K_d of 0.39 nM for D2 receptor and an orally available *5-HT-2* receptor antagonist.

HY-113008A

cis-Urocanic acid (Z)-Urocanic acid; cis-UCA	5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid is a **5-HT2A receptor** agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (K_d=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .

HY-111200

Vabicaserin hydrochloride 4 Publications Verification SCA 136	5-HT Receptor	Neurological Disease
Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT_2C) *receptor*-selective agonist with an EC₅₀ of 8 nM.

HY-103138

(Rac)-WAY-161503 hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease Metabolic Disease
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity **5-HT_2C receptor** agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .

HY-101094

Ocaperidone 1 Publications Verification R79598	5-HT Receptor Dopamine Receptor	Neurological Disease
Ocaperidone is an effective antipsychotic agent, acting as a potent *5-HT₂* and dopamine D₂ antagonist, and a 5-HT_1A agonist, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT₂, a₁-adrenergic receptor, dopamine D₂, histamine H₁ and a₂-adrenergic receptor, respectively, and a pEC₅₀ and pK_i of 7.60 and 8.08 for h5-HT_1A.

HY-B2089

Cinitapride	5-HT Receptor Dopamine Receptor	Neurological Disease Metabolic Disease
Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a *5-HT2* and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .

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-145393

5-HT2A receptor agonist-1	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-1 (Compound 3) is a selective **5-HT2A receptor** agonist with the EC₅₀ of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders .

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-103102

TCB2 1 Publications Verification	5-HT Receptor	Neurological Disease
TCB2 is an agonist of serotonin *5-HT_2A* receptor.

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-100993

α-Methylserotonin maleate	5-HT Receptor	Cardiovascular Disease
α-Methylserotonin maleate is a potent and selective agonist of **5-HT₂ receptor*. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor*-mediated phosphoinositide hydrolysis .

HY-19950

5-HT2A receptor agonist-6	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-6 (compound 47) is a selective *5-HT_2A* receptor agonist (pEC₅₀=6.58) .

HY-19686

Ipsapirone TVX Q 7821 free base	5-HT Receptor	Neurological Disease
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT_1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT_1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT₂ and the α₁-adrenergic function .

HY-100330

YM348 1 Publications Verification	5-HT Receptor	Metabolic Disease
YM348 is a potent and orally active **5-HT_2C receptor** agonist, which shows a high affinity for cloned human **5-HT_2C receptor (K_i**: 0.89 nM).

HY-103138A

(Rac)-WAY-161503 1 Publications Verification	5-HT Receptor	Neurological Disease Metabolic Disease
(Rac)-WAY-161503 is a potent, selective, highly affinity **5-HT_2C receptor** agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects .

HY-123838

Ro60-0175	5-HT Receptor	Neurological Disease
Ro60-0175 is a potent and selective agonist of *5-HT_2C* receptor. Ro60-0175 reduces self-administration .

HY-W077477

IHCH-7113	5-HT Receptor	Neurological Disease
IHCH-7113 (Compound 166) is an agonist of **5-HT2A serotonin receptor** with antidepressant activity. IHCH-7113 is promising for research of antipsychotic agent .

HY-145841

5-HT2A receptor agonist-2	5-HT Receptor	Cardiovascular Disease
5-HT2A receptor agonist-2 is a highly potent serotonin **5-HT2 receptor** agonists. 5-HT2A receptor agonist-2 inspires 5-HT_2A, 5-HT_2B, and 5-HT_2C with EC₅₀ values of 1.7, 0.58, and 0.50 nM, respectively .

HY-N4157

Isopteropodine	mAChR 5-HT Receptor Bacterial	Neurological Disease
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial** activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-175511

5-HT2A agonist 7	5-HT Receptor	Neurological Disease
5-HT2A agonist 7 (Compound 45) is an orally active and highly selective serotonin receptor 2A (5-HT_2A) agonist (EC₅₀=12 nM). 5-HT2A agonist 7 is promising for research of psychiatric disorders such as depression .

HY-133024

Flumexadol	5-HT Receptor	Neurological Disease
Flumexadol is a selective and affinity **5-HT_2C receptor** agonist with a K_i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT_2A receptor. Flumexadol is an orally active non-narcotic analgesic .

HY-126057

(R)-Praziquantel	Parasite 5-HT Receptor	Infection
(R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human **5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal** eutomer .

HY-179063

5-HT2A receptor agonist-13	5-HT Receptor Dopamine Receptor Serotonin Transporter	Neurological Disease
5-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the **5-HT_2A receptor, with an EC₅₀ value of 416.9 nM and a K_i** value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the **5-HT_2B receptor (EC₅₀** = 120.2 nM), D2 receptor (K_i = 1298 nM), and has no activity towards the 5-HT_2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC₅₀ = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD) .

HY-175657

5-HT2A receptor agonist-12	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-12 (compound 161-2) is a potent *5-HT2A* agonist with an EC₅₀ value of <100 nM for h5-HT2A .

HY-101100

Anpirtoline hydrochloride D-16949 hydrochloride	5-HT Receptor	Neurological Disease
Anpirtoline (D-16949) hydrochloride is a centrally acting 5-HT_1B receptor agonist, with K_is of 28 nM (5-HT_1B), 150 nM (5-HT_1A) and 1.49 μM (5-HT2). Anpirtoline hydrochloride has serotonergic, antinociceptive, antidepressant-like effects .

HY-175822

5-HT2A inverse agonist-1	5-HT Receptor	Neurological Disease
5-HT2A inverse agonist-1 is a *5-HT_2A* receptor inverse agonist with a IC₅₀ of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease .

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-175515

5-HT2C agonist-11	5-HT Receptor	Neurological Disease
5-HT2C agonist-11 (Compound 1) is an orally active, brain-penetrant and selective **5-HT_2C receptor** agonist (EC₅₀=15 nM). 5-HT2C agonist-11 activates the Gq protein signaling pathway, promoting intracellular calcium release. 5-HT2C agonist-11 is promising for research of depression, post-traumatic stress disorder (PTSD) and neuropathic pain .

HY-14546R

Aripiprazole (Standard) OPC-14597 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Infection Neurological Disease Inflammation/Immunology
Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at *5-HT2B* and *5-HT2A* receptors and displays partial agonist actions at 5-HT1A, *5-HT2C, D3, and D4 receptors*. Aripiprazole can be used for the research of schizophrenia and COVID19 .

HY-14546S

Aripiprazole-d8 OPC-14597-d₈	5-HT Receptor	Neurological Disease
Aripiprazole-d₈ (OPC-14597-d₈) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

HY-161511

LPH-5	5-HT Receptor	Neurological Disease
LPH-5 is a selective *5-HT2A* receptor agonist (EC₅₀=190 nM). LPH-5 works by selectively activating the *5-HT2A* receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the *5-HT2A* receptor. LPH-5 can be used to further explore the *5-HT2A* receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders .

HY-156532C

(-)-5-HT2C agonist-3	5-HT Receptor	Neurological Disease
(-)-5-HT2C agonist-3 (compound (-)-19) is a *5-HT_2C* selective agonist with G_q signaling preference, with EC₅₀ values for *5-HT₂* receptors of *5-HT_2C: 103 nM; 5-HT_2B: 570 nM; 5-HT_2A: 72 nM. (-)-5-HT2C* agonist-3 can be used in antipsychotic research .

HY-162423

CYB210010	5-HT Receptor Androgen Receptor	Neurological Disease
CYB210010 is an orally bioavailable, long-acting serotonin *5-HT2* receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC₅₀: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration .

HY-169786

5-HT2A receptor agonist-5	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-5 (compound I-3) is a potent *5-HT2A* receptor agonist with a K_i value of 0.017 µM. 5-HT2A receptor agonist-5 shows antidepressant activity .

HY-172978

5-HT2A receptor agonist-8	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-8 (compound 8) is a potent **5-HT2A receptor** agonist with an EC₅₀ of 0.6784 nM. 5-HT2A receptor agonist-8 can be used in the study of depressive disorders and bipolar disorders .

HY-172980

5-HT2A receptor agonist-9	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-9 (Compound 9) is a β-arrestin-biased **5-HT_2A receptor** agonist. 5-HT2A receptor agonist-9 can be used in the research of neurological diseases such as antidepressant and psychedelic .

HY-174909

5-HT2A receptor agonist-11	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-11 (Compound I-69) is a *5-HT2A* receptor agonist with an EC₅₀ of 22 nM. 5-HT2A receptor agonist-11 can be used in the research of mental illness or central nervous system disorders .

HY-169785

7-Methyl DMT 7-TMT	5-HT Receptor	Neurological Disease
7-Methyl DMT (7-TMT) is a *5-HT2* receptor agonist. Structurally, 7-Methyl DMT is a tryptamine derivative. It can be used as an analytical reference standard for the psychoactive substance DOM. 7-Methyl DMT is also used in research in the field of neurological diseases .

HY-176721

5-HT2A receptor agonist-10	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-10 (Compound (R)-I-121.HCl) is a **5-HT2A receptor** agonist, with an IC₅₀ of 2192.39 nM for h5-HT2A and h5-HT1A, respectively. 5-HT2A receptor agonist-10 can be used for the research of psychosis, mental illnesses and CNS disorders .

HY-173269

5-HT2A receptor agonist-7	5-HT Receptor	Others
5-HT2A receptor agonist-7 (517) is a *5-HT2A* modulator, with an EC₅₀ of <100 nM .

HY-B2089R

Cinitapride (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease Metabolic Disease
Cinitapride (Standard) is the analytical standard of Cinitapride. This product is intended for research and analytical applications. Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a *5-HT2* and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .

HY-108400

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

Cat. No.	Product Name	Type

HY-100993

α-Methylserotonin maleate	Biochemical Assay Reagents
α-Methylserotonin maleate is a potent and selective agonist of **5-HT₂ receptor*. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor*-mediated phosphoinositide hydrolysis .

HY-15401A

WAY 163909 (hydrochloride)

Biochemical Assay Reagents

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

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0049

Nuciferine 5+ Cited Publications	Alkaloids Aporphine Alkaloids other families Plants Isoquinoline Alkaloids Source Classification	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-17038

Agomelatine Maximum Cited Publications 9 Publications Verification S-20098	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-N0247

Saikosaponin B1 2 Publications Verification	Structural Classification Classification of Application Fields Umbelliferae Plants Disease Research Fields Saccharides Monosaccharides Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification Cancer	Hedgehog Smo STAT Interleukin Related TNF Receptor
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the **5-HT_2C receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer** activities thus can be studies in research for cancers such as Medulloblastoma (MB) .

HY-N4157

Isopteropodine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	mAChR 5-HT Receptor Bacterial
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial** activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-17038A

Agomelatine hydrochloride Maximum Cited Publications 9 Publications Verification S-20098 hydrochloride	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-N8200

Cassiaside B2	Monophenols Classification of Application Fields Phenols Caesalpiniaceae Cassia obtusifolia (L.) H. S. Irwin & Barneby Plants Inflammation/Immunology Disease Research Fields Source Classification	Phosphatase Monoamine Oxidase 5-HT Receptor
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a *5-HT2C* receptor agonist . ..

HY-17038B

Agomelatine (L(+)-Tartaric acid) Maximum Cited Publications 9 Publications Verification S-20098 L(+)-Tartaric acid	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine L(+)-Tartaric acid is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-17038R

Agomelatine (Standard) S-20098 (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-N4157R

Isopteropodine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	Reference Standards mAChR 5-HT Receptor Bacterial
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial** activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-N0049R

Nuciferine (Standard)	Alkaloids other families Plants Source Classification	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.

HY-17038AR

Agomelatine hydrochloride (Standard) S-20098 hydrochloride (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite Reference Standards
Agomelatine (hydrochloride) (Standard) is the analytical standard of Agomelatine (hydrochloride). This product is intended for research and analytical applications. Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-N0247R

Saikosaponin B1 (Standard)	Structural Classification Umbelliferae Plants Saccharides Monosaccharides Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification	Reference Standards Smo
Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the *5-HT_2C* receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .

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-126057S

(R)-Praziquantel-d11
(R)-Praziquantel-d₁₁ is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer .

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-W052508S

Norquetiapine-d8

Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .

HY-14546S

Aripiprazole-d8

Aripiprazole-d₈ (OPC-14597-d₈) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

HY-17038S2

Agomelatine-d3
Agomelatine-d₃ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

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-17038S1

Agomelatine-d4
Agomelatine-d₄ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-15296S1

Cabergoline-d6
Cabergoline-d₆ is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).

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-W744750

TDHL-d10
TDHL-d₁₀ (Tergurid-d₁₀; Terguride-d₁₀; trans-Dihydrolisuride-d₁₀) is the deuterium labeled TDHL (HY-12714). TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.

HY-113008AS

cis-Urocanic acid-13C3
cis-Urocanic acid- ¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .

HY-176436S

GW-117
GW-117 is a **5-HT2C receptor** antagonist and a melatonin (MT1/MT2) receptor agonist. GW-117 shows antidepressant-like and anxiolytic-like 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 .

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-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-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-14153AS

Tegaserod-13C,d3 maleate
Tegaserod- ¹³C,d₃ (maleate) is the ¹³C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract .

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-15296S

Cabergoline-d5
Cabergoline-d₅ is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, 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-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-135392S

N-Desmethyl Pimavanserin-d9 hydrochloride
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively .

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-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-100658S

Didesmethyl cariprazine-d8

Didesmethyl cariprazine-d₈ is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (K_i: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.

Cat. No.	Product Name		Classification

HY-172995

RS130-180		Alkynes
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT_2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .

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