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Isoforms Recommended:	α-1 microglobulin 5-HT₂ Receptor

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5-HT 2A receptor

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By Targets:	5-HT Receptor (37) COX (2) Dopamine Receptor (8) GlyT (3) Isotope-Labeled Compounds (2) P2X Receptor (3) Reference Standards (4) Serotonin Transporter (1) Transthyretin (TTR) (2)
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Targets Recommended: 5-HT Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N1957

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

HY-14557A

Pimavanserin hemitartrate Maximum Cited Publications 12 Publications Verification ACP-103 hemitartrate	5-HT Receptor	Neurological Disease
Pimavanserin (ACP-103) hemitartrate is a potent and brain-penetrant5-HT 2A receptor inverse agonist with pIC₅₀ and pK_i of 8.73 and 9.3, respectively.

HY-A0019A

Paliperidone palmitate 1 Publications Verification 9-Hydroxyrisperidone palmitate	Dopamine Receptor 5-HT Receptor	Neurological Disease
Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-109067A

Opiranserin hydrochloride VVZ-149 hydrochloride	GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .

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-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-109067

Opiranserin VVZ-149	GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .

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-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-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-101622

5-HT6/7 antagonist 1	5-HT Receptor Dopamine Receptor	Neurological Disease
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes *5-HT6/7/2A* and D2 receptors, without interacting with M1 receptors and hERG channels.

HY-W1123900

5-HT2A agonist 3	5-HT Receptor	Neurological Disease
5-HT2A agonist 3 (Compound P-141) is a selective 5-hydroxytryptamine 2A receptor (5-HT_2A) agonist with an EC₅₀ value of 13.80 nM. 5-HT2A agonist 3 is promising for research of mental illnesses such as depression, post-traumatic stress disorder, obsessive-compulsive disorder, and central nervous system disorders .

HY-175285

5-HT2AR-IN-1	5-HT Receptor	Neurological Disease
5-HT_2AR-IN-1 (Compound Ie) is an orally active 5-hydroxytryptamine 2A receptor (5-HT_2AR) inhibitor with antidepressant efficacy. 5-HT_2AR-IN-1 reduces 5-HT_2AR expression and SERT protein levels. 5-HT_2AR-IN-1 is promising for research of central nervous system (CNS), such as depression and addiction-related disorders .

HY-A0019AS

Paliperidone palmitate-d4 9-Hydroxyrisperidone palmitate-d₄	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-165527

S18327	Dopamine Receptor 5-HT Receptor	Neurological Disease
S18327 is a multi-target antipsychotic agent. S18327 exerts its efficacy by acting on multiple neurotransmitter systems in the brain, and it has antagonistic effects on dopamine receptors (particularly the D2 receptor) and 5-hydroxytryptamine 2A receptors (5-HT2A *receptor). S18327 can counteract excessive dopamine activity and hypo-function of glutamate. S18327 exhibits a multi-parameter pharmacological profile that is highly similar to that of Clozapine (HY-14539). S18327 can produce the same discriminative stimulus as Clozapine, improve cognitive filtering deficits associated with schizophrenia, and display anxiolytic properties. S18327 has relatively weak affinity for histaminergic receptors* and muscarinic receptors, which avoids the side effects of Clozapine .

HY-N1957R

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

HY-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-117792

LY314228	5-HT Receptor	Inflammation/Immunology
LY314228 is an aminoguanidine *5-HT2* antagonist with relative selectivity for *5-HT2A receptors* (IC50: 147.9 nM). The Ki values of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .

HY-16567S

Asenapine-13C,d3 hydrochloride Org 5222-13C,d3 hydrochloride	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
Asenapine- ¹³C,d₃ (hydrochloride) is the ¹³C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.

HY-14557AR

Pimavanserin hemitartrate (Standard) ACP-103 hemitartrate (Standard)	5-HT Receptor Reference Standards	Neurological Disease
Pimavanserin hemitartrate (Standard) is the analytical standard of Pimavanserin hemitartrate. This product is intended for research and analytical applications. Pimavanserin (ACP-103) hemitartrate is a potent and brain-penetrant 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.

HY-14148

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

HY-A0019AR

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

HY-121574

RU 27849	5-HT Receptor	Others
RU 27849 (Compound 27) is a **5-HT receptor** 2A agonist, and can be used to study tryptamine recognition site binding .

HY-146077

5-HT6/5-HT2A receptor ligand-2	5-HT Receptor	Neurological Disease
5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties .

HY-146076

5-HT6/5-HT2A receptor ligand-1	5-HT Receptor	Neurological Disease
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research .

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-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-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-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-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-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-W681014

5-Fluoro-α-methyltryptamine hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
5-Fluoro-α-methyltryptamine hydrochloride may cause an increase in intracellular levels of 5-HT followed by an increase in 5-HT release. 5-Fluoro-α-methyltryptamine hydrochloride exhibits EC₅₀ values of 37 nM, 14 nM, 78 nM and 8.47 nM for DA, 5HT, NE and 5-HT2A, respectively .

HY-109067AR

Opiranserin hydrochloride (Standard) VVZ-149 hydrochloride (Standard)	Reference Standards GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin hydrochloride (Standard) is the analytical standard of Opiranserin (hydrochloride) (HY-109067A). This product is intended for research and analytical applications. Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .

HY-134483

5-HT7/5-HT2A receptor antagonist 1	5-HT Receptor	Neurological Disease
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pK_i = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1957

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

HY-N1957R

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

Species:	Human (2)
Tag:	His (2) Flag (2)
Source:	Sf9 insect cells (2)

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P703149

	5HT2A Protein, Human (S162K, M164W, sf9, Flag, His) HTR2; HTR2A; Serotonin receptor 2A	Human	Sf9 insect cells
	5HT2A Protein, Human (S162K, M164W, sf9, Flag, His) is the recombinant human-derived 5HT2A, expressed by sf9 insect cells, with His, Flag labeled tag.,

HY-P703150

	5HT2A Protein, Human (L247A, L371A, sf9, Flag, His) HTR2; HTR2A; Serotonin receptor 2A	Human	Sf9 insect cells
	5HT2A Protein, Human (L247A, L371A, sf9, Flag, His) is the recombinant human-derived 5HT2A, expressed by sf9 insect cells, with His, Flag labeled tag.,

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HY-A0019AS

Paliperidone palmitate-d4

Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .