Uses
GR 113808 has been used as a serotonin receptor 4 (5-HT4R) blocker to study its effects on the calcium (Ca
2+) transients in rat ventricular cardiomyocytes. It has also been used as a 5-HT4R antagonist to study its effects on
de novo enteric neurogenesis in post-embryonic zebrafish.
Definition
ChEBI: An indolyl carboxylate ester obtained by formal condensation between the carboxy group of 1-methylindole-3-carboxylic acid with the hydroxy group of N-{2-[4-(hydroxymethyl)piperidin-1-yl]ethyl}methanesulfonamide.
Biological Activity
Potent, selective 5-HT 4 receptor antagonist (pK B = 9.43 in human colonic muscle, and K d = 0.15 nM for binding to cloned human 5-HT 4 receptors). Displays > 300-fold selectivity over 5-HT 1A , 5-HT 1B , 5-HT 2A , 5-HT 2C and 5-HT 3 receptors.
Biochem/physiol Actions
GR 113808 is a 5-HT4 serotonin receptor antagonist.
