5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

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

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.

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.

ML 10302 hydrochloride is a specific agonist 5-HT4 and binds 5-HT receptors with Kis of 1.07 nM and 782 nM for 5-HT4 and 5-HT3.

PF-03382792 is a small molecule 5-HT4 receptor activator for the study of Alzheimer's disease.

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).

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.

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

Tegaserod maleate (SDZ-HTF-919) is a 5-HT4 agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation. Its use was the only drug approved by the United States Food and Drug Administration to help relieve the abdominal discomfort, bloating and constipation associated with irritable bowel syndrome. On March 30, 2007, the U.S. Food and Drug Administration requested that Novartis withdraw Zelnorm from shelves. The FDA alleges a relationship between prescriptions of the drug and increased risks of heart attack or stroke.

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.

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.

Mosapride Citrate is a 5-HT4 receptor agonist used to stimulate gastrointestinal motility via acetylcholine. Mosapride Citrate facilitates acetylcholine release from the enteric cholinergic neurons.

Fabesetron (FK1052) is an orally active compound that acts as a dual antagonist, targeting both the 5-HT3 and 5-HT4 receptors. It exhibits efficacy in studying emesis induced by cancer chemotherapy, showing potential for managing both acute and delayed symptoms.

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

DSP-6952 is a 5-HT4 receptor partial agonist, inhibiting visceral hypersensitivity and ameliorating gastrointestinal dysfunction.

GR 125487 sulfamate is a 5-HT4 receptor antagonist.

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

RS 100235 is a 5-HT4 Serotonin Receptor.

Prucalopride hydrochloride is a selective agonist of the 5-HT4.

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

Des-4-fluorobenzyl Mosapride, the main metabolite of mosapride, acts as a gastroprokinetic agent improving upper gastrointestinal (GI) motility by stimulating the serotonin receptor 4 (5-HT4; EC50= 74.2 nM, in guinea pig ileal longitudinal muscle myenteric plexus). It has been shown to increase colonic motility in dogs, horses, and guinea pigs in vivo. Mosapride, including this metabolite, is utilized in human and veterinary medicine to mitigate post-surgical and Parkinson's-induced constipation.

SB 207710 is a selective and high affinity antagonist of 5-HT4 receptor.

Indeloxazine HCl acts as a serotonin releasing agent, norepinephrine reuptake inhibitor, and NMDA receptor antagonist. Indeloxazine hydrochloride is an antidepressant and cerebral activator. It has been found to enhance acetylcholine release in the rat fo

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.

BIMU-1 is an agonist of 5-HT4 receptor.

Potent and selective 5-HT4 receptor antagonist

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.

Cisapride tartrate is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be e......

ML 10302 is a potent5-HT4 receptor agonist (Ki = 1.07 nM) that induces significant prokinesia both in the small bowel and colon by activating the cholinergic pathways. ML 10302 also shows the potential in neurology diseases research [1].

Renzapride is a 5-HT3 antagonist and 5-HT4 agonist. Renzapride also functions as a 5-HT2B antagonist and has some affinity for the 5-HT2A and 5-HT2C receptors.

Piboserod (SB-207266) (SB 207266) is a selective 5-HT(4) receptor antagonist.

SUVN-D4010 is an effective, selective, brain penetrant, and orally active agonist of 5-HT4 receptor partially used to treat Alzheimer's disease and other dementia-related cognitive dysfunction.

RS 67333 hydrochloride (RO5203648) is a potent, selective partial agonist of the 5-HT4 receptor (5-HT4R) with a pKi value of 8.7 in guinea-pig striatum. It demonstrates lower binding affinities for other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1 and D2, and muscarinic M1-M3 receptors. Notably, RS 67333 hydrochloride exhibits neuroprotective properties, rendering it useful in Alzheimer's disease research.

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.

SB 203186 hydrochloride is a potent 5-HT4 receptor antagonist

(S)-Renzapride ((S)-BRL 24924), an isomer of Renzapride, acts as a 5-HT4 receptor agonist with a K_i value of 115 nM and also antagonizes 5HT2b and 5HT3 receptors. It is utilized in studies focused on constipation-predominant irritable bowel syndrome (C-IBS).

VRX 03011, a 5-HT4 partial agonist, is used potentially for the treatment of Alzheimer's disease.

SB 271046 hydrochloride (SB 271046A) is selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.35, 6.55, 6.27 at 5-HT6, 5-HT1A, 5-HT1D and D3, and 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. It increases extracellular aspartate and glutamate in the frontal cortex and exhibits anticonvulsant activity (EC50: 0.16 μM).

Usmarapride (SUVN-D4010) is a selective, orally active, potent 5-HT4 receptor partial agonist with blood-brain barrier permeability and an EC50 value of 44 nM. Usmarapride (SUVN-D4010) can be used to study cognitive deficits associated with Alzheimer's disease.

5-HT3/5-HT4 receptor antagonist

ML 10375 is an antagonist of 5-HT4 receptor.

Velusetrag(TD-5108)is an effective, selective, and highly potent agonist of the 5-HT4 receptor, and being developed for the treatment of gastroparesis, chronic constipation, and irritable bowel syndrome.

Relenopride, a 5-HT agonist, is used potentially for the treatment of chronic constipation.

Capeserod HCl, a 5-hydroxytriptamine 4 (5-HT4) receptor agonist, is used potentially for the treatment of Alzheimer's disease.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

potent and selective 5-HT4 antagonist

SC 53116 Hydrochloride is selective agonist of the newly identified serotonin 5-HT4 receptor subtype.