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.

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

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.

Lintopride HCl is a 5HT-4 antagonist.

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

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.

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

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

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.

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.

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.

Tegaserod is an orally available 5-HT4R agonist and 5-HT2B receptor antagonist with inhibitory effects on various 5-hydroxytryptamine receptors. Tegaserod has antitumor activity and is used in the treatment of irritable bowel syndrome (IBS).

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.

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

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.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

Oxazolone has been used as a haptenizing agent to induce inflammatory responses in intestinal tissue of adult zebrafish and as a model for gene expression studies in two forms of inflammatory bowel disease, such as Crohn's disease and ulcerative colitis.

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

Exendin-4 (Exenatide) is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.