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Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists
Authors:Wang Y  Chackalamannil S  Hu Z  Clader J W  Greenlee W  Billard W  Binch H  Crosby G  Ruperto V  Duffy R A  McQuade R  Lachowicz J E
Affiliation:Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. yuguang.wang@spcorp.com
Abstract:Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acetylcholine release after oral administration.
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