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5-HT2B antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (65) Adrenergic Receptor (1) Apoptosis (3) Autophagy (1) Dopamine Receptor (9) Drug Derivative (1) Drug Isomer (1) G protein-coupled Bile Acid Receptor 1 (2) Histamine Receptor (3) Isotope-Labeled Compounds (5) Melatonin Receptor (3) Orexin Receptor (OX Receptor) (3) P2X Receptor (3) Parasite (1) Reference Standards (12) Sigma Receptor (2) Sodium Channel (4) TRP Channel (2)
By Research Areas:	Cancer (6) Cardiovascular Disease (9) Endocrinology (7) Inflammation/Immunology (6) Metabolic Disease (9) Neurological Disease (48)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 Maximum Cited Publications 10 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-N0049

Nuciferine 5+ Cited Publications	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-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-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-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-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-10895A

SB-334867 free base Maximum Cited Publications 10 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-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-107836

Methiothepin mesylate 2 Publications Verification 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-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-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-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-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-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-121675

2-Bromo-LSD BOL-148; Bromolysergide	5-HT Receptor G protein-coupled Bile Acid Receptor 1	Neurological Disease
2-Bromo-LSD (BOL-148) is a blood-brain barrier-permeable 5-HT_2A partial agonist and competitive partial antagonist. 2-Bromo-LSD acts as both a potent partial agonist (with an EC₅₀ of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a K_B of 0.18 nM for Gq dissociation) at the 5-HT_2A receptor. 2-Bromo-LSD exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT_2A. 2-Bromo-LSD lacks *5-HT_2B* agonist activity. 2-Bromo-LSD induces dendritogenesis and spinogenesis. 2-Bromo-LSD reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .

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-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-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-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-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-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-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-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-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-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-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-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 .

HY-125784B

(S)-Viloxazine hydrochloride (S)-Viloxazin hydrochloride; (S)-Emovit hydrochloride	Drug Isomer Adrenergic Receptor	Neurological Disease
(S)-Viloxazine hydrochloride is the isomer of Viloxazine hydrochloride (HY-125784). Viloxazine hydrochloride is the hydrochloride salt form of Viloxazine (HY-W380450). Viloxazine (Viloxazin) hydrochloride is a norepinephrine reuptake inhibitor and a potent 5-HT_2C agonist agent and *5-HT_2B* antagonist，EC₅₀ for 5-HT_2C b> is 32 μM，and the IC₅₀ for 5-HT_2B is 27 μM. Viloxazine hydrochloride's mechanism of action primarily involves serotonergic and noradrenergic pathways. Viloxazine hydrochloride is used in antidepressant 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-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-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-10564R

Sarpogrelate hydrochloride (Standard) MCI-9042 (Standard)	Reference Standards 5-HT Receptor	Cardiovascular Disease
Sarpogrelate (hydrochloride) (Standard) is the analytical standard of Sarpogrelate (hydrochloride). This product is intended for research and analytical applications. 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-101009

Methiothepin maleate Metitepine maleate; Ro-8-6837 maleate	5-HT Receptor	Neurological Disease
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-111491

Methiothepin Metitepine; Ro 8-6837	5-HT Receptor	Neurological Disease
Methiothepin (Metitepine; Ro 8-6837) 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-119946

BF-1	5-HT Receptor	Neurological Disease
BF-1 is a 5-HT_2B receptor antagonist with a pK_i value of 10.05 and an IC₅₀ value of 2.6 nM .

HY-18596

SB-215505	5-HT Receptor	Neurological Disease
SB-215505 is an orally active 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-103153R

SB 204741 (Standard)	Reference Standards 5-HT Receptor	Cardiovascular Disease
SB 204741 (Standard) is the analytical standard of SB 204741. This product is intended for research and analytical applications. SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1 .

HY-171195

VU0631019	5-HT Receptor	Metabolic Disease
VU0631019 is a potent antagonist of *5-HT_2B, with the IC₅₀* of 29 nM. VU0631019 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .

HY-171194

VU0530244	5-HT Receptor	Metabolic Disease
VU0530244 is a potent antagonist of *5-HT_2B, with the IC₅₀* of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .

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-100851

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

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 .

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-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-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 .

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-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-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-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.

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