5-ht4 agonist

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

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

DA-6886 is an agonist 5-Hydroxytryptamine receptor 4 (5-HT4). DA-6886 induced 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 revealed that it inhibited hERG channel current with an pIC50 value of 4.3, indicating that the compound was 1000-fold more selective for the 5-HT4 receptor over hERG channels.

Minesapride, a novel 5-hydroxytryptamine 4 (5-HT4) receptor partial agonist, is a potential gastrointestinal prokinetic agent for the treatment of irritable bowel syndrome with constipation.

Renzapride (BRL 24924) is a mixed 5-hydroxytryptamine type 4 (5-HT4) agonist and 5-HT3 receptor antagonist.Renzapride can be used in the study of constipation-predominant irritable bowel syndrome (C-IBS).

Capeserod is a potential 5-HT4 receptor (5-hydroxytryptamine receptor 4) agonist for the study of digestive disorders and neurological disorders.

Norcisapride is a 5-hydroxytryptamine receptor 3 (5-HT3) and (5-hydroxytryptamine receptor 4 (5-HT4) dual agonist used for the treatment of gastrointestinal disorders, orofacial disorders, and otorhinolaryngologic disorders.

Relenopride (YKP 10811) is a selective 5-HT4 receptor agonist that promotes intestinal motility and is used in the study of intestinal disorders.

Tryptamine hydrochloride is a monoamine alkaloid, metabolite of tryptophan and CNS active substance, agonist of 5-HT4 receptor, TAAR1 and AHR, with potential for blood-brain barrier permeability.

Metoclopramide (5-Chloro-2-methoxyprocainamide) is a dopamine D2 antagonist which has been used for treatment of a variety of gastrointestinal symptoms over the last thirty years. In various countries, metoclopramide is the antiemetic drug of choice in pregnant women. Findings provide reassurance regarding the safety of metoclopramide for the fetus when the drug is given to women to relieve nausea and vomiting during pregnancy. Evidence also supports its use for gastroparesis (poor stomach emptying) and gastroesophageal reflux disease. It appears to bind to dopamine D2 receptors where it is a receptor antagonist, and is also a mixed 5-HT3 receptor antagonist/ 5-HT4 receptor agonist.

Felcisetrag (TD-8954) is a potent and selective orally active 5-HT4 agonist with gastrointestinal prokinetic properties.Felcisetrag shows high affinity for the human recombinant 5-HT4(c) (h5-HT4(c)) receptor with a pKi of 9.4.

Prucalopride Succinate (Resolor Succinate) is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively.

Tegaserod maleate (SDZ-HTF-919) is a 5-HT4 agonist manufactured by Novartis for managing irritable bowel syndrome and constipation. It was the only drug approved by the United States Food and Drug Administration for relieving abdominal discomfort, bloating, and constipation associated with irritable bowel syndrome. On March 30, 2007, the FDA requested that Novartis withdraw Zelnorm from the market due to alleged increased risks of heart attack or stroke associated with its use.

Revexepride is a highly selective agonist of the 5-HT4 receptor and a potential inducer of CYP3A4 enzyme. Revexepride is used for the treatment of gastroesophageal reflux disease.

Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.

VRX 03011 (also known as NTC-942 and PRX-03140) is a 5-HT4 partial agonist with potential applications in the treatment of Alzheimer's disease.

TD-2749 is a selective 5-HT4 agonist discovered by Theravance through multivalent compound design as part of a compound discovery project aimed at finding new treatments for gastrointestinal motility disorders. It is primarily used to treat chronic constipation, constipation-predominant irritable bowel syndrome (C-IBS), opioid-induced constipation, functional dyspepsia, and diabetic gastroparesis.

THRX-194556 is an agonist of the 5-HT4 receptor. It is applicable in the study of gastrointestinal functional disorders and Alzheimer's disease.

5-HT4R agonist-2 (Compound 4) is a selective 5-HT4 receptor agonist with an EC50 of 0.41 nM. This compound significantly enhances intestinal and colonic transit, increases stool output and moisture content, while maintaining minimal systemic absorption, making it a promising candidate for research in chronic idiopathic constipation.

MR33317 is an inhibitor of acetylcholinesterase with an IC50 value of 41 nM. Additionally, it acts as an agonist for brain 5-HT4 receptors.

Cinitapride (Blaston) is a gastroprokinetic agent. It slows the actions of the muscles to reduce the symptoms of conditions such as acid reflux, delayed gastric emptying, and ulcer dyspepsia. Cinitapride acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors.

Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors

Cisapride acts directly as a selective agonist of serotonin 5-HT4 receptor with IC50 value of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

CJ 033466 is a selective partial agonist of 5-HT4 receptor (EC50 = 9 nM) with gastroprokinetic effect.