5-ht4 receptor

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

Sulamserod (RS 100302) is a potent 5-HT4 receptor antagonist with antiarrhythmic activity for the study of atrial fibrillation and cardiovascular related diseases.

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.

PF-04995274 is an effective, high-affinity, and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. PF-04995274 has an EC50 range of 0.26-0.47 nM for hu

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.

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.

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

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.

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.

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.

potent and selective 5-HT4 antagonist

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.

RS-67333 is a selective and efficient partial agonist of the 5-HT4 receptor (5-HT4R) with neuroprotective effects, useful in preventing amyloid deposition and behavioral deficits in the 5XFAD mouse model of Alzheimer's disease.

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

SC-53116 HCl can increase the production of serotonin in central nervous system tissues and is a psychoactive agent.

Usmarapride free base (SUVN-D4010 free base) is a selective and orally active 5-HT4 receptor partial agonist, increasing soluble amyloid precursor protein α levels, useful in Alzheimer's disease research.

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.

Velusetrag hydrochloride is a biochemical.

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).

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

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, used to study cognitive deficits associated with Alzheimer's disease.