Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.

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

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

Kozlowski JA; Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA. joseph.kozlowski@spcorp.com

Bioorg Med Chem Lett ; 10(20): 2255-7, 2000 Oct 16.

Article in En | MEDLINE | ID: mdl-11055332

ABSTRACT

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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Collection: 01-internacional Database: MEDLINE Main subject: Benzene Derivatives / Receptors, Muscarinic / Muscarinic Antagonists Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2000 Document type: Article Affiliation country:

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