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serotonin 5-HT2 receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (106) Serotonin Transporter (7) Adrenergic Receptor (21) Androgen Receptor (1) Apoptosis (8) Autophagy (6) Bacterial (4) Dopamine Receptor (32) Drug Derivative (1) Drug Metabolite (5) DYRK (5) Environmental Pollutants (1) GABA Receptor (2) GlyT (3) GnRH Receptor (2) Histamine Receptor (2) Isotope-Labeled Compounds (8) Ligands for E3 Ligase (1) mAChR (10) Melatonin Receptor (2) Mitophagy (5) P-glycoprotein (6) P2X Receptor (6) Phosphatase (1) Phytohormone (1) Reference Standards (26) Sodium Channel (4) TRP Channel (2) Wnt (2)
By Research Areas:	Cancer (20) Cardiovascular Disease (11) Endocrinology (2) Inflammation/Immunology (6) Metabolic Disease (10) Neurological Disease (99)
Click Chemistry:	Alkynes (1)

118

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

GMP Molecules

Targets Recommended: 5-HT Receptor Serotonin Transporter

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0737A

Harmine 25+ Cited Publications Telepathine	DYRK 5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 nM .

HY-11018

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

HY-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-N0737

Harmine hydrochloride 25+ Cited Publications Telepathine hydrochloride	Environmental Pollutants DYRK 5-HT Receptor	Neurological Disease Cancer
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 nM .

HY-B1033

Metergoline 2 Publications Verification	5-HT Receptor Dopamine Receptor Sodium Channel	Neurological Disease
Metergoline is a **serotonin (5-HT) receptor** and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i of 16 nM. Metergoline is also a reversible neural Na ⁺ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .

HY-A0095

Flibanserin 2 Publications Verification BIMT-17; BIMT-17BS	5-HT Receptor	Neurological Disease Cancer
Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and **5-HT2A receptor antagonist with K_i** values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research ^- .

HY-B1213

Trimipramine maleate 1 Publications Verification	5-HT Receptor Bacterial	Neurological Disease
Trimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy .

HY-32329

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

HY-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-B1371

Spiperone 2 Publications Verification Spiroperidol	Dopamine Receptor 5-HT Receptor Wnt	Neurological Disease
Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT_1A, and serotonin *5-HT_2A* antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases .

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-B1107

Naftidrofuryl oxalate Nafronyl oxalate salt	5-HT Receptor	Cardiovascular Disease
Naftidrofuryl oxalate (Nafronyl oxalate salt) is an orally active 5-HT₂ receptor antagonist. Naftidrofuryl oxalate selectively blocks vascular and platelet 5-HT₂ receptors, inhibiting Serotonin (HY-B1473A)-induced vasoconstriction, platelet aggregation, and vascular smooth muscle cell proliferation. Naftidrofuryl oxalate can be used for the research of intermittent claudication, peripheral occlusive arterial disease, and critical limb ischaemia .

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-109112

Brilaroxazine RP5063	Dopamine Receptor 5-HT Receptor	Neurological Disease Inflammation/Immunology
Brilaroxazine (RP5603) is a potent and orally active multimodal *dopamine (DA)/serotonin* (5-HT)** modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .

HY-10457

Velusetrag TD-5108	5-HT Receptor	Neurological Disease Metabolic Disease
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin *5-HT₄ receptor* (5-HT4R), with a pK_i** of 7.7. Velusetrag exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .

HY-B0102C

(R)-Fluoxetine hydrochloride	Serotonin Transporter	Neurological Disease
(R)-Fluoxetine hydrochloride, an antidepressant, is serotonin reuptake inhibitor (SSRI). (R)-Fluoxetine hydrochloride has modest affinity at the 5-HT_2A and 5-HT_2C receptors .

HY-100665

Dehydroaripiprazole 1 Publications Verification OPC-14857; DM-14857	5-HT Receptor Dopamine Receptor	Neurological Disease
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D₂/D₃ receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin 5-HT₁A, *5-HT₂A* and *5-HT₂B* receptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole .

HY-B1737

Pirenperone R 47465	5-HT Receptor	Neurological Disease
Pirenperone (R 47465) is a **5-HT₂ serotonin receptor** antagonist. Pirenperone exhibits modest anxiolytic activity .

HY-103102

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

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-10792A

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

HY-110232

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

HY-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-P3641A

Kisspeptin 13 TFA	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

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-G0002

Lurasidone metabolite 14326	Drug Metabolite Dopamine Receptor 5-HT Receptor	Neurological Disease
Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 can be used in the research of schizophrenia and bipolar depression .

HY-10457A

Velusetrag hydrochloride TD-5108 hydrochloride	5-HT Receptor	Neurological Disease Metabolic Disease
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin *5-HT₄ receptor* (5-HT₄R), with a pK_i** of 7.7. Velusetrag hydrochloride exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .

HY-124821

VA012	5-HT Receptor	Neurological Disease Metabolic Disease
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin *5-HT_2C* receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .

HY-105285

Piromelatine 2 Publications Verification Neu-P11	Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel	Neurological Disease
Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and **serotonin 5-HT_2B** antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities .

HY-32329A

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

HY-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-W016194

1-(Carboxymethyl)cyclohexanecarboxylic acid 1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E; Gabapentin Related Compound E	5-HT Receptor	Neurological Disease
1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.

HY-N0737AR

Harmine (Standard) Telepathine (Standard)	Reference Standards DYRK 5-HT Receptor	Neurological Disease Cancer
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .

HY-N0737AG

Harmine Telepathine	DYRK 5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 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-A0095A

Flibanserin hydrochloride (propan-2-ol) hydrate 2 Publications Verification BIMT-17 hydrochloride (propan-2-ol) hydrate; BIMT-17BS hydrochloride (propan-2-ol) hydrate	5-HT Receptor	Neurological Disease Cancer
Flibanserin (BIMT-17) hydrochloride (propan-2-ol) hydrate is an orally active serotonin 5-HT1A receptor agonist and **5-HT2A receptor antagonist with K_i** values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride (propan-2-ol) hydrate binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin hydrochloride (propan-2-ol) hydrate shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research ^- .

HY-B1213A

Trimipramine	5-HT Receptor Bacterial	Neurological Disease
Trimipramine is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .

HY-11018B

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

HY-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-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-118557

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

HY-101755

Tedatioxetine hydrobromide Lu AA24530 hydrobromide	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and *5-HT_2A, 5-HT_2C, 5-HT₃* and α_1A-adrenergic receptor antagonist . ,

HY-172995

RS130-180	5-HT Receptor	Neurological Disease
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 .

HY-14827

Zicronapine Lu 31-130	Dopamine Receptor 5-HT Receptor	Neurological Disease
Zicronapine is an antipsychotic agent with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2A receptors .

HY-14827A

Zicronapine fumarate Lu 31-130 fumarate	Dopamine Receptor 5-HT Receptor	Neurological Disease
Zicronapine (Lu 31-130) fumarate is an antipsychotic agent with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine (Lu 31-130) fumarate has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2A receptors .

HY-116680

LY53857	5-HT Receptor	Cardiovascular Disease Neurological Disease
LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated *5-HT₂* receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .

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-11018S2

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

HY-121311

Metrenperone	Serotonin Transporter Adrenergic Receptor	Cardiovascular Disease
Metrenperone is an inhibitor for **5-HT2 receptor*. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin*-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue .

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-N0737AG

Harmine

Telepathine

Biochemical Assay Reagents

Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM .

Cat. No.	Product Name	Target	Research Area

HY-P3641A

Kisspeptin 13 TFA	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0737A

Harmine 25+ Cited Publications Telepathine	Alkaloids Zygophyllaceae Peganum harmala Linn. Plants Indole Alkaloids Source Classification	DYRK 5-HT Receptor
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 nM .

HY-N0737

Harmine hydrochloride 25+ Cited Publications Telepathine hydrochloride	Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Plants Indole Alkaloids Source Classification	Environmental Pollutants DYRK 5-HT Receptor
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 nM .

HY-N0737AR

Harmine (Standard) Telepathine (Standard)	Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Plants Indole Alkaloids Source Classification	Reference Standards DYRK 5-HT Receptor
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .

HY-N0737AG

Harmine Telepathine	Alkaloids Zygophyllaceae Peganum harmala Linn. Plants Indole Alkaloids Source Classification	DYRK 5-HT Receptor
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 nM .

HY-N0737R

Harmine hydrochloride (Standard) Telepathine hydrochloride (Standard)	Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Plants Indole Alkaloids Source Classification	Reference Standards DYRK 5-HT Receptor
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .

HY-N9418R

Gibberellin A5 (Standard)	Rosaceae Plants Rosa canina Gremli ex Christ Source Classification	Phytohormone Reference Standards
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .

Cat. No.	Product Name	Chemical Structure

HY-110232

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

HY-14541S

Olanzapine-d3
Olanzapine-d₃ (LY170053-d₃) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .

HY-11018S2

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

HY-11018S1

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

HY-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-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-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-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-14541S2

Olanzapine-d8

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

HY-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-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.

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 .

Targets Recommended: 5-HT Receptor Serotonin Transporter

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0737AG

Harmine Telepathine	DYRK 5-HT Receptor	Neurological Disease Inflammation/Immunology Cancer
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of **5-HT_2A serotonin receptor, with an K_i** of 397 nM .

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