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Isoforms Recommended:	5-HT₄ Receptor

Results for "

5-HT4 Receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (62) Apoptosis (6) Autophagy (4) Cholinesterase (ChE) (2) Cytochrome P450 (1) Dopamine Receptor (2) Drug Metabolite (1) Endogenous Metabolite (2) Isotope-Labeled Compounds (3) mAChR (1) P2X Receptor (1) Potassium Channel (2)
By Research Areas:	Cancer (12) Cardiovascular Disease (8) Endocrinology (1) Inflammation/Immunology (5) Metabolic Disease (16) Neurological Disease (41)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-101341

RS 67333 hydrochloride	5-HT Receptor	Neurological Disease
RS 67333 hydrochloride is a potent and selective **5-HT4 receptor (5-HT4R) partial agonist with a pK_i** of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .

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-110094

BIMU 8	5-HT Receptor	Neurological Disease
BIMU 8 is a potent and selective *5-HT4* agonist with EC₅₀s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors .

HY-15574

Piboserod 3 Publications Verification SB-207266	5-HT Receptor	Cardiovascular Disease
Piboserod (SB 207266) is a 5-HT4 selective inhibitor of the serotonin receptor.

HY-103134

SB 204070A	Others	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-B2089R

Cinitapride (Standard)	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-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-123747

SC-53116	5-HT Receptor	Neurological Disease
SC-53116 is a selective *5-HT4* receptor agonist with EC₅₀ at 23 nM .

HY-123747A

SC-53116 hydrochloride	5-HT Receptor	Neurological Disease
SC-53116 hydrochloride is a selective *5-HT4* receptor agonist with EC₅₀ at 23 nM .

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-109065

Minesapride	5-HT Receptor	Others
Minesapride is a partial agonist with a highly selective serotonin 4 (5-HT4) receptor. Minesapride enhances gastrointestinal peristalsis and colon transport by activating the *5-HT4* receptor. Minesapride increases bowel movements and suppresses visceral allergic reactions. Minesapride can be used in the study of constipation-type irritable bowel syndrome (IBS-C) .

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-14441

ML 10302	5-HT Receptor	Neurological Disease
ML 10302 is a potent agonist *5-HT4* receptor with K_i of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases .

HY-16729

Relenopride YKP10811	5-HT Receptor	Metabolic Disease
Relenopride is a agonist of novel potent 5-HT₄ receptor partial with weak binding to 5-HT 2B receptors (K_i = 31 nM) .

HY-103108

CJ033466	5-HT Receptor	Metabolic Disease
CJ033466 is a novel and selective **5-HT₄ receptor partial agonist with an EC₅₀** of 9 nM and has gastroprokinetic effect .

HY-102057

Felcisetrag TD-8954	5-HT Receptor	Others
Felcisetrag (TD-8954) is an orally active, potent and selective *5-HT₄* receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pK_i =9.4) for human 5-HT_4(c) receptors.

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-162591

MR33317	Cholinesterase (ChE) 5-HT Receptor	Neurological Disease
MR33317 is an inhibitor of acetylcholinesterase with an IC₅₀ value of 41nM. MR33317 is also an agonist at brain *5-HT₄ receptors* .

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-121826

Naronapride ATI-7505	5-HT Receptor	Metabolic Disease Inflammation/Immunology
Naronapride (ATI-7505) is a potent prokinetic **5-HT₄ receptor** agonist. Naronapride can be used for gastrointestinal diseases research .

HY-U00373

Revexepride	5-HT Receptor Cytochrome P450	Neurological Disease
Revexepride is a highly selective **5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme**, used for the treatment of gastroesophageal reflux disease.

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-16729A

Relenopride hydrochloride YKP10811 hydrochloride	5-HT Receptor	Inflammation/Immunology
Relenopride (YKP10811) hydrochloride is a specific and selective **5-HT₄ receptor agonist (K_i*=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT_2A (K_i=600 nM) and 5-HT_2B receptors* (K_i=31 nM) than for 5-HT₄. Relenopride hydrochloride increases gastrointestinal (GI) motility .

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-14442

ML 10302 hydrochloride	5-HT Receptor	Neurological Disease Metabolic Disease
ML 10302 hydrochloride is a potent and selective **5-HT₄ receptor agonist, with an EC₅₀ of 4 nM. ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT₃** receptor in binding assay .

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-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-124381

ML10375	Others	Others
ML10375 is a compound that modulates 5-HT4 and 5-HT2 receptors, affects gap junction coupling in rat atrial myocytes, and regulates intracellular cAMP concentration and L-type calcium current.

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-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-14149

Cisapride 1 Publications Verification R 51619; (±)-Cisaprid	5-HT Receptor Potassium Channel	Neurological Disease
Cisapride (R 51619) is an orally active *5-HT₄* receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a hERG blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

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-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-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-101653

MHP 133	Cholinesterase (ChE) mAChR 5-HT Receptor	Neurological Disease
MHP 133 is a agent with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with K_i of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.

HY-103137

Zacopride hydrochloride	5-HT Receptor	Neurological Disease
Zacopride hydrochloride is a highly potent 5-HT₃ receptor antagonist with K_is of 0.38 and 373 nM for 5-HT₃ and *5-HT₄* receptor, respectively. Zacopride hydrochloride is also a moderate I_K1 channel agonist. Zacopride hydrochloride exerts significant antiarrhythmic and cardiac protective effects .

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-116565

Usmarapride SUVN-D4010	5-HT Receptor	Neurological Disease
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant **5-HT₄ receptor partial agonist (EC₅₀**=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .

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-116565A

Usmarapride free base SUVN-D4010 free base	5-HT Receptor	Neurological Disease
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant **5-HT₄ receptor partial agonist (EC₅₀**=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .

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 5-HT (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .

HY-14152

Prucalopride hydrochloride	5-HT Receptor	Cancer
Prucalopride hydrochloride is an orally active, selective and specific **5-HT4 receptor agonist (high affinity), with pK_is of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor** signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .

HY-14149R

Cisapride (Standard)	5-HT Receptor Potassium Channel	Neurological Disease
Cisapride (Standard) is the analytical standard of Cisapride. This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active *5-HT₄* receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a hERG blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-14149A

Cisapride monohydrate R 51619 monohydrate; (±)-Cisaprid monohydrate	5-HT Receptor	Neurological Disease Metabolic Disease
Cisapride monohydrate is an orally and potent *5-HT₄* receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .

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-160921

Capeserod SL65.0155 free base	5-HT Receptor	Neurological Disease
Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a K_i of 0.6 nM for 5-HT₄ receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W015169

5-Methoxytryptamine O-Methylserotonin	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Indole Alkaloids Cancer	Drug Metabolite 5-HT Receptor Endogenous Metabolite
5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

HY-W015169A

5-Methoxytryptamine hydrochloride	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Indole Alkaloids Cancer	5-HT Receptor Endogenous Metabolite
5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .

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].

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 .

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