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5-HT2B receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (32) Apoptosis (2) Autophagy (1) Dopamine Receptor (4) Histamine Receptor (2) Isotope-Labeled Compounds (2) Melatonin Receptor (2) Orexin Receptor (OX Receptor) (2) P2X Receptor (2) Parasite (1) Sigma Receptor (2) Sodium Channel (2) TRP Channel (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (3) Endocrinology (5) Inflammation/Immunology (2) Metabolic Disease (6) Neurological Disease (26)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-15419

RS-127445 hydrochloride 2 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-18596

SB-215505	5-HT Receptor	Neurological Disease
SB-215505 is a potent and subtype-selective *5-HT_2B* receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively . SB-215505 increases wakefulness and motor activity in rats .

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-15419A

RS-127445
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-14153AS

Tegaserod-13C,d3 maleate SDZ-HTF-919-¹³C,d₃; HTF-919-¹³C,d₃	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease Metabolic Disease
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[1][2][5].

HY-14153

Tegaserod	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-100851A

LY-272015 hydrochloride
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-14153A

Tegaserod maleate SDZ-HTF-919; HTF-919	5-HT Receptor Apoptosis	Neurological Disease Metabolic Disease
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-103129A

SB-200646	5-HT Receptor	Neurological Disease
SB-200646 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-200646 is orally active and has electrophysiological and anxiolytic properties in vivo .

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-103155

SB-221284	5-HT Receptor	Neurological Disease
SB 221284 is a selective 5-HT_2C/2B receptor antagonist with pK_i values are 6.4, 7.9 and 8.6 for 5-HT_2A, *5-HT_2B* and 5-HT_2C receptors, respectively. SB 221284 can be used for the research of neurological disease .

HY-18099A

S1RA hydrochloride 1 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-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-10792

Eplivanserin SR-46349	5-HT Receptor	Neurological Disease
Eplivanserin (SR-46349) 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 displays >20-fold selectivity more selective for 5-HT_2A than 5-HT_2B and 5-HT_2C .

HY-103154

SB228357	5-HT Receptor	Neurological Disease
SB228357 is a selective, potent and orall active 5-HT_2C/2B receptor antagonist with pK_i values of 6.9, 8.0 and 9.0 for 5-HT_2A, *5-HT_2B* and 5-HT_2C, respectively. SB228357 has antidepressant/anxiolytic effects .

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-14147A

(S)-Renzapride (S)-BRL 24924	5-HT Receptor	Metabolic Disease
(S)-Renzapride ((S)-BRL 24924) is the isomer of HY-14147 Renzapride. Renzapride is a 5-HT₄ receptor agonist with a K_i value of 115 nM. Renzapride also is a *5HT2b* and 5HT3 receptor antagonist. Renzapride can be used for constipation predominant irritable bowel syndrome (C-IBS) study .

HY-18099

S1RA 1 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-B1033

Metergoline 1 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-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-101365A

RS-102221 hydrochloride	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-10895

SB-334867 5 Publications Verification 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-10895A

SB-334867 free base 5 Publications Verification 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-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 .

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-105285

Piromelatine 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-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-10564

Sarpogrelate hydrochloride 1 Publications Verification MCI-9042	5-HT Receptor	Cardiovascular Disease
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-10564S

Sarpogrelate-d3 hydrochloride MCI-9042-d₃	Isotope-Labeled Compounds 5-HT Receptor	Cardiovascular Disease
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[1][2][3].

HY-N0049

Nuciferine 4 Publications Verification	Parasite 5-HT Receptor Dopamine Receptor	Neurological Disease
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-134807

Indophagolin	P2X Receptor 5-HT Receptor Autophagy	Cancer
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC₅₀=140 nM). Indophagolin antagonizes the purinergic receptor P2X₄ as well as P2X₁ and P2X₃ with IC₅₀s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the G_q-protein-coupled P2Y₄, P2Y₆, and P2Y₁₁ receptors (IC₅₀s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT₆ (IC₅₀=1.0 μM) and a moderate effect on receptors 5-HT_1B, 5-HT_2B, 5-HT_4e, and 5-HT₇ .

HY-N0049R

Nuciferine (Standard)	5-HT Receptor Dopamine Receptor	Neurological Disease
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and *5-HT_2B* (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-101009

Methiothepin maleate Metitepine maleate; Ro-8-6837 maleate
Methiothepin maleate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

HY-107836

Methiothepin mesylate Metitepine mesylate; Ro 8-6837 mesylate	5-HT Receptor	Neurological Disease
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

HY-106136

TIK-301 PD-6735; LY-156735	Melatonin Receptor 5-HT Receptor	Neurological Disease
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT₁ and MT₂ receptors agonist with K_is of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a **5-HT_2B/5-HT_2C receptors** antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0049

Nuciferine 4 Publications Verification	Structural Classification Alkaloids Aporphine Alkaloids other families Source classification Plants Isoquinoline Alkaloids	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)	Structural Classification Alkaloids other families Source classification Plants	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-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[1][2][5].

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[1][2][3].

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[1][2][3].

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