GR 113808

• CAT Number: I007022
• CAS Number: 144625-51-4
• Molecular Formula: C19H27N3O4S
• Molecular Weight: 393.5
• Purity: ≥95%
• Target: 5-HT Receptor
• Solubility: Soluble in DMSO
• Storage: Store at RT
• IUPAC Name: [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-methylindole-3-carboxylate
• InChI: 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
• InChIKey: MOZPSIXKYJUTKI-UHFFFAOYSA-N
• SMILES: CN1C=C(C2=CC=CC=C21)C(=O)OCC3CCN(CC3)CCNS(=O)(=O)C

GR 113808 (Cat.No:I007022) is a potent, selective 5-HT4 receptor antagonist (pKB = 9.43 in human colonic muscle, and Kd = 0.15 nM for binding to cloned human 5-HT4 receptors). GR 113808 displays > 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.

Reference

1:Effect of the intracerebroventricular administration of GR 113808, a selective 5-HT4 antagonist, on water intake during hyperosmolarity and hypovolemia. Castro L, Varjão B, Silva I, Duque B, Batista A, Santana R, Luz P, Rocha MA Jr, Fregoneze JB, De Castro-e-Silva E.Braz J Med Biol Res. 2001 Jun;34(6):791-6. PMID: 11378670 Free Article2:Pharmacological comparison between [3H]GR 113808 binding sites and functional 5-HT4 receptors in neurons. Ansanay H, Sebben M, Bockaert J, Dumuis A.Eur J Pharmacol. 1996 Mar 7;298(2):165-74. PMID: 8867105 3:Characterization of [3H]GR 113808 binding to 5-HT4 receptors in brain tissues from patients with neurodegenerative disorders. Wong EH, Reynolds GP, Bonhaus DW, Hsu S, Eglen RM.Behav Brain Res. 1996;73(1-2):249-52. PMID: 8788512 4:Intranigral GR-113808, a selective 5-HT4 receptor antagonist, attenuates morphine-stimulated dopamine release in the rat striatum. Pozzi L, Trabace L, Invernizzi R, Samanin R.Brain Res. 1995 Sep 18;692(1-2):265-8. PMID: 8548313 5:Blockade of human atrial 5-HT4 receptors by GR 113808. Kaumann AJ.Br J Pharmacol. 1993 Nov;110(3):1172-4. PMID: 8298805 Free PMC Article