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Results for "

5-HT2B

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (126) Adrenergic Receptor (6) Apoptosis (3) Autophagy (6) Dopamine Receptor (24) Dopamine Transporter (1) Drug Derivative (2) Drug Isomer (1) Drug Metabolite (1) G protein-coupled Bile Acid Receptor 1 (2) GABA Receptor (1) GPR68 (1) Histamine Receptor (6) Isotope-Labeled Compounds (8) mAChR (3) MCHR1 (GPR24) (2) Melatonin Receptor (3) Orexin Receptor (OX Receptor) (3) P2X Receptor (3) Parasite (3) Reference Standards (23) Serotonin Transporter (2) Sigma Receptor (4) Small Interfering RNA (siRNA) (3) Sodium Channel (4) TRP Channel (2)
By Research Areas:	Cancer (14) Cardiovascular Disease (16) Endocrinology (12) Infection (5) Inflammation/Immunology (12) Metabolic Disease (21) Neurological Disease (101)
Oligonucleotides:	Rat Pre-designed siRNA Sets (1) Mouse Pre-designed siRNA Sets (1) Human Pre-designed siRNA Sets (1) siRNAs (3)

144

Inhibitors & Agonists

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-15296

Cabergoline Maximum Cited Publications 12 Publications Verification FCE-21336	Dopamine Receptor Autophagy	Endocrinology Cancer
Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and *5-HT_2B* receptors (K_i=0.7, 1.5, and 1.2, respectively).

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-10895

SB-334867 5+ Cited Publications SB 334867A	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 (SB 334867A) is an excellent,selective and blood-brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .

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-15419

RS-127445 hydrochloride 3 Publications Verification	5-HT Receptor	Neurological Disease
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .

HY-103153

SB 204741 1 Publications Verification	5-HT Receptor	Cardiovascular Disease
SB 204741 is a selective and high affinity *5-HT_2B* antagonist with a pK_i value of 7.1 .

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-W380450

Viloxazine Viloxazin; Emovit	5-HT Receptor	Neurological Disease
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC₅₀= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes *5-HT2B* receptors (K_i=4.2 μM) and agonizes 5-HT2C receptors (EC₅₀= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .

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-125784

Viloxazine hydrochloride Viloxazin hydrochloride; Emovit hydrochloride	5-HT Receptor	Neurological Disease
Viloxazine hydrochloride is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC₅₀=0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes *5-HT2B* receptors (K_i=4.2 μM) and agonizes 5-HT2C receptors (EC₅₀=32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD) .

HY-10895A

SB-334867 free base 5+ Cited Publications SB334867A free base	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .

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_is 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-10559

Nelotanserin 2 Publications Verification APD125	5-HT Receptor	Neurological Disease Cancer
Nelotanserin is a potent 5-HT_2A inverse agonist, a moderately potent 5-HT_2C partial inverse agonist and a weak *5-HT_2B* inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

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-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-101369

BW-723C86 1 Publications Verification	5-HT Receptor	Cardiovascular Disease Neurological Disease
BW-723C86 is an orally active and a selective 5-HT_2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats. BW-723C86 dilates pulmonary arteries and inhibits liquid meal-induced gastric accommodation .

HY-101365A

RS-102221 hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (K_i=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats .

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-15419A

RS-127445 3 Publications Verification	5-HT Receptor	Neurological Disease
RS-127445 is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .

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-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-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-B1101A

Pimethixene maleate Pimetixene maleate	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .

HY-103129

SB-200646A	5-HT Receptor	Neurological Disease
SB-200646A is the first selective *5-HT_2B/2C* over 5-HT_2A receptor antagonist with pK_i values of 7.5, 6.9 and 5.2 for *5-HT_2B, 5-HT_2C* and 5-HT_2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo .

HY-103094

LY266097 hydrochloride	5-HT Receptor	Inflammation/Immunology
LY266097 hydrochloride is a selective *5-HT2B* receptor antagonist with pK_is of 7.7, 9.8, and 7.6 for 5-HT2A, *5-HT2B, 5-HT2C, respectively. 5-HT2B* receptor blockade contributes to the research in depression .

HY-147203

5-HT2B antagonist-1	5-HT Receptor	Cardiovascular Disease Metabolic Disease Endocrinology Cancer
5-HT2B antagonist-1 is an orally active *5-HT2B* receptor antagonist with an IC₅₀ value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease .

HY-100851A

LY-272015 hydrochloride	5-HT Receptor	Cardiovascular Disease
LY-272015 hydrochloride is an orally active, specific 5-HT_2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .

HY-118010A

(+)-Norfenfluramine hydrochloride d-Norfenfluramine hydrochloride	5-HT Receptor	Cardiovascular Disease
(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective *5-HT_2B* receptor agonist (K_i: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca ²⁺. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease .

HY-W131725

(+)-Norfenfluramine d-Norfenfluramine	5-HT Receptor	Cardiovascular Disease
(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective *5-HT_2B* receptor agonist (K_i: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca ²⁺. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease .

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-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-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-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-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-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-15296R

Cabergoline (Standard) FCE-21336 (Standard)	Reference Standards Dopamine Receptor Autophagy	Endocrinology Cancer
Cabergoline (Standard) is the analytical standard of Cabergoline. This product is intended for research and analytical applications. 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-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-15419R

RS-127445 hydrochloride (Standard)	5-HT Receptor	Neurological Disease
RS-127445 (hydrochloride) (Standard) is the analytical standard of RS-127445 (hydrochloride). This product is intended for research and analytical applications. RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .

HY-110129

Eplivanserin hemifumarate SR-46349 hemifumarate; SR 46349B	5-HT Receptor	Neurological Disease
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT_2A receptor antagonist, with an IC₅₀ of 5.8 nM in rat cortical membrane, and a K_d of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT_2A than 5-HT_2B and 5-HT_2C .

HY-101365

RS-102221	5-HT Receptor	Neurological Disease
RS-102221 is a selective 5-HT2C receptor antagonist (K_i=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats .

HY-172258

5-HT2B antagonist-2	5-HT Receptor	Cancer
5-HT2B antagonist-2 (Compound 19c) is a *5HT_2B* receptor antagonist with an IC₅₀ of 1.09 nM. 5-HT2B antagonist-2 can downregulate the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, and significantly reduce the deposition of fibrosis, thereby reducing the fibrotic area and inhibiting the fibrotic process in CCl4-induced liver fibrosis mouse models. 5-HT2B antagonist-2 can be used in the study of immune inflammatory-related diseases, particularly in the research of pulmonary fibrosis diseases .

HY-W014208

NGX-267 AF-267B	mAChR	Others
NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors .

HY-W296398

5-Bromo-N,N-dimethyltryptamine 5-Bromo-N,N-DMT	5-HT Receptor Drug Metabolite	Neurological Disease
5-Bromo-N,N-dimethyltryptamine, an active metabolite, is an antidepressant and sedative drug lead. 5-Bromo-N,N-dimethyltryptamine shows strong affinity towards 5-HT_1A, 5-HT_2B, 5-HT₆, and 5-HT₇ .

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-14147

Renzapride BRL 24924	5-HT Receptor	Metabolic Disease
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT₄ receptor agonist with a K_i value of 115 nM. Renzapride (BRL 24924) is also a *5HT2b* and 5HT3 receptor antagonist . Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study .

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-B1101

Pimethixene Pimetixene	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .

Cat. No.	Product Name	Type

HY-15401A

WAY 163909 hydrochloride

Biochemical Assay Reagents

WAY-163909 hydrochloride is a potent 5-hydroxytryptamine receptor 2C (5-HT2C) agonist with an EC50 of 8 nM and a maximum efficacy of 90%, while displaying minimal activity at 5-HT2A receptors. Its selectivity is further demonstrated by Ki values of 10.5 nM for 5-HT2C, alongside higher Ki values for 5-HT2A (212 nM), 5-HT7 (343 nM), and 5-HT2B (485 nM), and it lacks significant activity at various other receptors.

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-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.

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-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-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-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-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-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-10564S

Sarpogrelate-d3 hydrochloride

Sarpogrelate-d₃ (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .

HY-10564S1

Sarpogrelate-d4 hydrochloride

Sarpogrelate-d₄ (MCI-9042-d₄) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT₂R antagonist, with pK_is of 8.52, 6.57, and 7.43 for 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT₁, 5-HT₃, 5-HT₄, α₁-, α₂- and β-adrenoreceptor, histamine H₁, H₂ and muscarinic M₃ receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .

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.

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.

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