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Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor
Authors:Kozlowski J A  Lowe D B  Guzik H S  Zhou G  Ruperto V B  Duffy R A  McQuade R  Crosby G  Taylor L A  Billard W  Binch H  Lachowicz J E
Affiliation:Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA. joseph.kozlowski@spcorp.com
Abstract:
Structure activity studies on [4-(phenylsulfonyl)phenyl]methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4-methoxyphenyl(S)-sufinyl]phenyl]-1-pi perazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned human M2 receptor was 2.7 nM; the M1/M2 selectivity is 40-fold.
Keywords:
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