Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor |
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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 |
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Affiliation: | Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA. joseph.kozlowski@spcorp.com |
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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. |
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