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HomeProduct name listGR 113808

GR 113808

Synonym(s):1-[2-[(Methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate;5-HT₄ Serotonin Receptor Antagonist, GR113808, GR 113808, GR-113808;GR113808 - CAS 144625-51-4 - Calbiochem

GR 113808 Structural

What is GR 113808?

The Uses of GR 113808

GR 113808 has been used as a serotonin receptor 4 (5-HT4R) blocker to study its effects on the calcium (Ca2+) 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.

What are the applications of Application

GR 113808 is a robust and selective receptor antagonist of SR-4

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.

Storage

Store at RT

Properties of GR 113808

Boiling point: 572.3±53.0 °C(Predicted)
Density  1.30±0.1 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: 44 mg/mL, soluble
form  solid
pka 11.22±0.40(Predicted)
color  white

Safety information for GR 113808

Computed Descriptors for GR 113808

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