GR113808

GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4. It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM). GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 µM in rabbit thoracic aorta and rat cerebral cortex, respectively). It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 µM for all). GR113808 inhibits relaxation induced by 5-HT (Cay-14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine, Cay-14486, pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.Formal Name: 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester. CAS Number: 144625-51-4. Molecular Formula: C19H27N3O4S. Formula Weight: 393.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 100 mM, Ethanol: 10 mM. lambdamax: 216, 290 nm. SMILES: CN1C=C(C(OCC2CCN(CCNS(C)(=O)=O)CC2)=O)C3=CC=CC=C31. InChi Code: InChI=1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3. InChi Key: MOZPSIXKYJUTKI-UHFFFAOYSA-N.