- Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
Bioorganic & medicinal chemistry letters (2000-10-31)
J A Kozlowski, D B Lowe, H S Guzik, G Zhou, V B Ruperto, R A Duffy, R McQuade, G Crosby, L A Taylor, W Billard, H Binch, J E Lachowicz
PMID11055332
要旨
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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