Diphenyl sulfoxides as selective antagonists of the muscarinic M 2 receptor

…, VB Ruperto, RA Duffy, R McQuade, G Crosby…

文献索引：Kozlowski, Joseph A; Lowe, Derek B.; Guzik, Henry S.; Zhou, Guowei; Ruperto, Vilma B.; Duffy, Ruth A.; McQuade, Robert; Crosby Jr., Gordon; Taylor, Lisa A.; Billard, William; Binch III, Herbert; Lachowicz, Jean E. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 20 p. 2255 - 2257

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被引用次数: 13

摘要

Structure–activity studies on [4-(phenylsulfonyl) phenyl] methylpiperazine led to the discovery of 4-cyclohexyl-α-[4-[[4-methoxyphenyl](S)-sulfinyl] phenyl]-1- piperazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned human M2 receptor was 2.7 nM; the M1/M2 selectivity is 40-fold.