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Isoforms Recommended:	α-1 microglobulin 5-HT₂ Receptor

Results for "

human 5-HT2B receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (25) Adrenergic Receptor (3) Apoptosis (3) Dopamine Receptor (5) GABA Receptor (1) Isotope-Labeled Compounds (3) Parasite (2) Reference Standards (2) Sigma Receptor (2)
By Research Areas:	Cancer (3) Infection (2) Inflammation/Immunology (1) Metabolic Disease (4) Neurological Disease (20)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-18099

S1RA 3 Publications Verification E-52862	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) is a highly selective *σ1 receptor* (σ1R) antagonist with K_i*s of 17 nM and 23.5 nM for human* σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .

HY-18099A

S1RA hydrochloride 3 Publications Verification E-52862 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >1000 nM). S1RA hydrochloride is a human *5-HT2B* receptor antagonist with an IC₅₀ value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .

HY-100658

Didesmethyl cariprazine	5-HT Receptor Dopamine Receptor	Neurological Disease
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-HT_1A receptor, and antagonist at the human *5-HT_2B* receptor (K_i: 1.41 nM (human D_2L), 0.056 nM (human D₃), 1.7 nM (human 5-HT_1A), 0.52 nM (human 5-HT_2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .

HY-15543A

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

HY-118301

ADX71441	GABA Receptor 5-HT Receptor	Neurological Disease
ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABA_B receptor. ADX71441 potentiates the activity of endogenous GABA at GABA_B receptor, with an EC₅₀ of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT_2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .

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-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-103135

SB 206553 hydrochloride	5-HT Receptor	Neurological Disease
SB 206553 hydrochloride is a high affinity, selective and orally active **5-HT_2B / 5-HT_2C receptor** antagonist (rat 5-HT_2B pA2 = 8.89, human 5-HT_2C pKi = 7.92) . SB 206553 possesses anxiolytic-like properties .

HY-126057S

(R)-Praziquantel-d11	Parasite 5-HT Receptor	Infection
(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-103110

ST1936 1 Publications Verification	5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor .

HY-178760

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

HY-15401

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

HY-15543

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

HY-123480

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

HY-103110A

ST1936 oxalate	5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 oxalate is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 oxalate also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor .

HY-14153S

Tegaserod-d11	5-HT Receptor Apoptosis Isotope-Labeled Compounds	Metabolic Disease Cancer
Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active *serotonin receptor* 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B** receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-123480A

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

HY-100658S

Didesmethyl cariprazine-d8	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
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.

HY-100658R

Didesmethyl cariprazine (Standard)	5-HT Receptor Reference Standards Dopamine Receptor	Neurological Disease
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. 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 (Ki: 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 .

HY-103110R

ST1936 (Standard)	Reference Standards 5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 (Standard) is the analytical standard of ST1936 (HY-103110). This product is intended for research and analytical applications. ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .

HY-100656AS

Desmethyl cariprazine-d8	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
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.

HY-181613

5-HT2A&5-HT2C agonist-3	5-HT Receptor	Neurological Disease
5-HT2A&5-HT2C agonist-3 (compound 4e) is an orally bioavailable and blood-brain barrier penetrant agonist of 5-HT2A and 5-HT2C. 5-HT2A&5-HT2C agonist-3 increases intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used for the research of neuropsychiatric disorders .

Cat. No.	Product Name	Chemical Structure

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-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 .

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-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.

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.

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.

Desmethyl cariprazine-d8

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

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