Discovery of N-{1-[3-(3-oxo-2, 3-dihydrobenzo [1, 4] oxazin-4-yl) propyl] piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist …

…, CT Christoffersen, B Bang-Andersen

Index: Sams, Anette G.; Hentzer, Morten; Mikkelsen, Gitte K.; Larsen, Krestian; Bundgaard, Christoffer; Plath, Niels; Christoffersen, Claus T.; Bang-Andersen, Benny Journal of Medicinal Chemistry, 2010 , vol. 53, # 17 p. 6386 - 6397

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Citation Number: 25

Abstract

The discovery and structure− activity relationship (SAR) of a series of allosteric muscarinic M1 receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as an agonist at the muscarinic M1 receptor across a panel of muscarinic receptor subtypes. Furthermore, 17 displayed a high degree of selectivity when tested in a broad panel of G-protein-coupled ...