Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists |
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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 |
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Affiliation: | Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. yuguang.wang@spcorp.com |
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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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