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5-HT4 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (39) Apoptosis (3) Autophagy (1) Dopamine Receptor (2) Isotope-Labeled Compounds (4) P2X Receptor (1) Reference Standards (4)
By Research Areas:	Cancer (6) Cardiovascular Disease (14) Endocrinology (1) Inflammation/Immunology (4) Metabolic Disease (8) Neurological Disease (22)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100170

5-HT4 antagonist 1	5-HT Receptor	Neurological Disease
5-HT4 antagonist 1 is a **5-HT₄ receptor** antagonist with a pK_i of 9.6.

HY-15574

Piboserod 4 Publications Verification SB-207266	5-HT Receptor	Cardiovascular Disease
Piboserod is an orally available selective antagonist of the **5-HT4 receptor*, with a K_i value of approximately 0.1 nM for human 5-HT4* receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .

HY-103134

SB 204070A	5-HT Receptor	Inflammation/Immunology
5-HT4 antagonist 3 hydrochloride is a highly selective 5-hydroxytryptamine receptor (5-HT₄) antagonist. 5-HT4 antagonist 3 (hydrochloride) blocks muscarine receptors and sodium channels. 5-HT4 antagonist 3 (hydrochloride) can be used to evaluate function of 5-HT₄ receptor .

HY-101668

Sulamserod RS-100302	5-HT Receptor	Cardiovascular Disease
Sulamserod is a **5-HT4 receptor** antagonist, with antiarrhythmic activities.

HY-15574A

Piboserod hydrochloride SB-207266 hydrochloride	5-HT Receptor	Cardiovascular Disease
Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.

HY-135439

SB-203186	5-HT Receptor	Neurological Disease
SB-203186 is a highly selective 5-HT₄ receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pK_B value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .

HY-101668A

Sulamserod hydrochloride RS-100302 hydrochloride	5-HT Receptor	Inflammation/Immunology
Sulamserod hydrochloride is a *5-HT4* receptor antagonist. Sulamserod hydrochloride can be used in gastrointestinal disease related research .

HY-15574R

Piboserod (Standard)	5-HT Receptor	Cardiovascular Disease
Piboserod (Standard) is the analytical standard of Piboserod. This product is intended for research and analytical applications. Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .

HY-103143A

SDZ 205-557	5-HT Receptor	Neurological Disease
SDZ 205-557 is a selective **5-HT₄ receptors** antagonist. SDZ 205-557 can be used for neurological research .

HY-103143

SDZ 205-557 hydrochloride	5-HT Receptor	Neurological Disease
SDZ 205-557 hydrochloride is a selective **5-HT₄ receptors** antagonist. SDZ 205-557 hydrochloride can be used for neurological research .

HY-101638

(±)-Fabesetron hydrochloride (±)-FK1052	5-HT Receptor	Neurological Disease
(±)-Fabesetron hydrochloride ((±)-FK1052) is the racemate of Fabesetron hydrochloride, which is a potent 5-HT3 and *5-HT4* receptor dual antagonist .

HY-101638A

(±)-Fabesetron (±)-FK1052 free base	5-HT Receptor	Neurological Disease
(±)-Fabesetron ((±)-FK1052 free base) is the racemate of Fabesetron, which is a potent 5-HT3 and *5-HT4* receptor dual antagonist .

HY-19927A

DA-6886 monohydrochloride	5-HT Receptor	Neurological Disease Endocrinology
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a *5-HT4* receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC₅₀ value of 4.3, indicating that the compound is 1000-fold more selective for the *5-HT4* receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .

HY-105201A

Fabesetron hydrochloride FK1052	5-HT Receptor	Neurological Disease Cancer
Fabesetron (FK1052) hydrochloride is an orally active 5-HT₃ receptor antagonist with **5-HT₄ receptor** antagonistic activity. Fabesetron hydrochloride can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .

HY-105201

Fabesetron FK1052 free base	5-HT Receptor	Neurological Disease Cancer
Fabesetron (FK1052) is an orally active 5-HT₃ receptor antagonist with **5-HT₄ receptor** antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy .

HY-117574

SB 207710	5-HT Receptor	Cardiovascular Disease
SB 207710 is a highly selective antagonist of the 5-HT4 receptor that has been shown to effectively block the positive inotropic effect induced by serotonin in human right atrial appendage preparations .

HY-101222

SB-203186 hydrochloride	5-HT Receptor	Cardiovascular Disease Neurological Disease
SB-203186 hydrochloride is a potent, selective and competitive *5-HT₄* antagonist. SB-203186 hydrochloride antagonizes the 5-HT₄ receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pK_B values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .

HY-44132

Dehydro Palonosetron RS 42358-197	5-HT Receptor	Neurological Disease
Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors .

HY-B2089

Cinitapride	5-HT Receptor Dopamine Receptor	Neurological Disease Metabolic Disease
Cinitapride is a nonselective 5-HT1 and **5-HT4 receptors agonist and a 5-HT2** and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .

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-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-101172

RS 23597-190 EP-A-501322	5-HT Receptor	Cardiovascular Disease
RS 23597-190 (EP-A-501322) is a high affinity and selective **5-HT4 receptor** antagonist. RS 23597-190 inhibits Serotonin (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .

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-B2089R

Cinitapride (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease Metabolic Disease
Cinitapride (Standard) is the analytical standard of Cinitapride. This product is intended for research and analytical applications. Cinitapride is a nonselective 5-HT1 and **5-HT4 receptors agonist and a 5-HT2** and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .

HY-103137R

Zacopride hydrochloride (Standard)	Reference Standards 5-HT Receptor	Cardiovascular Disease Neurological Disease
Zacopride (hydrochloride) (Standard) is the analytical standard of Zacopride (hydrochloride). This product is intended for research and analytical applications. Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist with Kis of 0.38 and 373 nM for 5-HT3 and 5-HT4 receptor, respectively. Zacopride hydrochloride is also a moderate IK1 channel agonist. Zacopride hydrochloride exerts significant antiarrhythmic and cardiac protective effects .

HY-118317

Zacopride	5-HT Receptor	Cardiovascular Disease Neurological Disease
Zacopride is an orally active 5-HT₃ receptor (K_i of 0.38 nM) antagonist and *5-HT₄* receptor (K_i of 373 nM) agonist. Zacopride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety .

HY-103137

Zacopride hydrochloride	5-HT Receptor	Cardiovascular Disease Neurological Disease
Zacopride hydrochloride is an orally active 5-HT₃ receptor (K_i of 0.38 nM) antagonist and *5-HT₄* receptor (K_i of 373 nM) agonist. Zacopride hydrochloride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride hydrochloride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety .

HY-101343

RS 39604	5-HT Receptor	Neurological Disease
RS 39604 is a potent, selective, and orally active **5-HT₄ receptor** antagonist with a pK_i of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pK_i<6.5) for 5-HT_1A, 5-HT_2C, 5-HT₃, α_1c, D₁, D₂, M₁, M₂, AT₁, B₁ and opioid mu receptors and moderate affinity for δ₁, (pK_i=6.8) and δ₂ (pK_i=7.8) sites .

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-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-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 .

HY-10564S1

Sarpogrelate-d4 hydrochloride MCI-9042-d₄	Isotope-Labeled Compounds 5-HT Receptor	Cardiovascular Disease
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-103152

GR 113808 Maximum Cited Publications 8 Publications Verification	5-HT Receptor	Neurological Disease Inflammation/Immunology
GR 113808 is a potent and highly selective *5-HT₄ receptor* antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors .

HY-103152R

GR 113808 (Standard)	Reference Standards 5-HT Receptor	Neurological Disease Inflammation/Immunology
GR 113808 (Standard) is the analytical standard of GR 113808. This product is intended for research and analytical applications. GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors .

HY-14153

Tegaserod 3 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-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-14153A

Tegaserod maleate 3 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-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 .

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-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 .

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 .

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-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 .

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