Discovery of N-(3-Fluorophenyl)-1-[(4-([(3 S)-3-methyl-1-piperazinyl] methyl) phenyl) acetyl]-4-piperidinamine (GSK962040), the First Small Molecule Motilin Receptor …

…, G Stemp, M Thompson, K Lawless…

Index: Westaway, Susan M.; Brown, Samantha L.; Fell, Stephen C. M.; Johnson, Christopher N.; MacPherson, David T.; Mitchell, Darren J.; Myatt, James W.; Stanway, Steven J.; Seal, Jon T.; Stemp, Geoffrey; Thompson, Mervyn; Lawless, Kirk; McKay, Fiona; Muir, Alison I.; Barford, Jonathan M.; Cluff, Chermaine; Mahmood, Sadhia R.; Matthews, Kim L.; Mohamed, Shiyam; Smith, Beverley; Stevens, Alexander J.; Bolton, Victoria J.; Jarvie, Emma M.; Sanger, Gareth J. Journal of Medicinal Chemistry, 2009 , vol. 52, # 4 p. 1180 - 1189

Full Text: HTML

Citation Number: 23

Abstract

N-(3-Fluorophenyl)-1-[(4-([(3 S)-3-methyl-1-piperazinyl] methyl) phenyl) acetyl]-4- piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the native rabbit motilin receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also ...