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Results for "

5HT4 Agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (50) Apoptosis (6) Autophagy (3) Cholinesterase (ChE) (2) Cytochrome P450 (4) Dopamine Receptor (3) Drug Derivative (1) Drug Isomer (1) Drug Metabolite (1) Isotope-Labeled Compounds (4) Potassium Channel (6)
By Research Areas:	Cancer (10) Endocrinology (1) Infection (1) Inflammation/Immunology (2) Metabolic Disease (18) Neurological Disease (36)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-101342

RS 67506 hydrochloride	5-HT Receptor	Neurological Disease
RS 67506 hydrochloride is a *5-HT4* receptor agonist. The pKi value of RS 67506 hydrochloride for *5-HT4* in guinea pig striatum is 8.8. RS 67506 hydrochloride can be used in neuro-related research .

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-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-HT*₄ receptors .

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-115774

5-HT4R agonist-1	Drug Derivative	Others
5-HT4R agonist-1 is an active compound.

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-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-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-100243

(+)-Norcisapride Ticalopride	5-HT Receptor	Neurological Disease
(+)-Norcisapride (Ticalopride) is a potent *5-HT4* agonist and a 5-HT3 antagonist. (+)-Norcisapride has activity in animals models of constipation .

HY-B0189S1

Mosapride-d5	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
Mosapride-d₅ is the deuterium labeled Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

HY-148846

Mosapride N-Oxide	Drug Metabolite	Metabolic Disease
Mosapride N-Oxide is a major active metabolite of Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT₄ agonist.

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-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-Z6430

Des-4-fluorobenzyl mosapride	5-HT Receptor	Neurological Disease
Des-4-fluorobenzyl mosapride is the primary metabolite of Mosapride (HY-B0189). Mosapride is an orally active gastroenterokinetic compound and is a 5HT4 agonist.

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-18138

PF-03382792	5-HT Receptor	Neurological Disease
PF-03382792 is a potent *5-HT₄* partial agonist with a K_i of 2.7 nM and an EC₅₀ of 0.9 nM for 5-HT_4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex .

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-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-128386

Cinitapride monotartrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Cinitapride monotartrate is a 5-HT_1A and *5-HT₄* agonist. Cinitapride monotartrate is also a 5-HT_2A and D₂ antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia .

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-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-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-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-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-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-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-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)	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-14149S

Cisapride-d6 R51619-d₆; (±)-Cisaprid-d₆	Isotope-Labeled Compounds 5-HT Receptor Potassium Channel	Neurological Disease
Cisapride-d₆ (R51619-d₆) is deuterium labeled Cisapride. 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-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-B0189

Mosapride 4 Publications Verification TAK-370; AS-4370	5-HT Receptor Cytochrome P450 Potassium Channel	Neurological Disease Cancer
Mosapride is an orally active gastroenterokinetic compound. Mosapride is a *5HT4* agonist. Mosapride is a CYP inducer. Mosapride has a concentration-dependent inhibitory effect on Kv4.3, and its IC₅₀ value is 15.2 μM. Mosapride can be used in the study of gastrointestinal diseases .

HY-B0189A

Mosapride citrate 4 Publications Verification TAK-370 citrate; AS-4370 citrate	5-HT Receptor Potassium Channel Cytochrome P450	Neurological Disease Cancer
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a *5HT4* agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC₅₀ value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases .

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-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-121249

Capeserod hydrochloride SL65.0155	5-HT Receptor	Neurological Disease
Capeserod hydrochloride (SL65.0155) is a *5-HT_4(e)* receptor partial agonist (K_i=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing *5-HT_4(b)* and *5-HT_4(e)* splice variants, stimulating cAMP production with IC₅₀ values ??of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia .

HY-B0189B

Mosapride citrate dihydrate TAK-370 citrate dihydrate; AS-4370 citrate dihydrate	5-HT Receptor Potassium Channel Cytochrome P450	Metabolic Disease Cancer
Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine₄ receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC₅₀ values of 15.2 μM . Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo .

HY-169825

(S)-PF-04995274	5-HT Receptor Drug Isomer	Neurological Disease
(S)-PF-04995274 is a partial agonist of the 5-hydroxytryptamine receptor 4 (5-HT₄R) and is an isomer of PF-04995274 (HY-18137) .

HY-168241

Flucopride	Cholinesterase (ChE) 5-HT Receptor	Infection
Flucopride (Compound 4a) is an AChE inhibitor (IC₅₀: 24 nM), and a partial 5-HT₄R agonist (K_i: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT₄R (EC₅₀: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .

HY-18137

PF-04995274	5-HT Receptor	Neurological Disease
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT₄R) agonist. PF-04995274 has an EC₅₀ range of 0.26-0.47 nM for human *5-HT_4A/4B/4D/4E* (K_i range of 0.15-0.46 nM), and has an EC₅₀ range of 0.59-0.65 nM for rat *5-HT_4S/4L/4E* (K_i of 0.30 nM for rat *5-HT_4S*). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .

HY-116266

RS 67333	Others	Others
RS 67333 is a 5-HT4R agonist with stress-preventive activity. RS 67333 attenuates stress-induced body weight changes and prevents depression- and anxiety-like behaviors in two mouse strains tested in different stress models.

HY-14151

Prucalopride 2 Publications Verification	5-HT Receptor Apoptosis Autophagy	Neurological Disease Cancer
Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pK_is of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .

HY-12694

Prucalopride succinate 2 Publications Verification R-108512	5-HT Receptor Apoptosis Autophagy	Metabolic Disease Cancer
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pK_is of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .

HY-14151R

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

Cat. No.	Product Name	Chemical Structure

HY-B0189S1

Mosapride-d5
Mosapride-d₅ is the deuterium labeled Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

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-14149S

Cisapride-d6
Cisapride-d₆ (R51619-d₆) is deuterium labeled Cisapride. 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-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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