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  • Title: Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
    Author: Kozlowski JA, Lowe DB, Guzik HS, Zhou G, Ruperto VB, Duffy RA, McQuade R, Crosby G, Taylor LA, Billard W, Binch H, Lachowicz JE.
    Journal: Bioorg Med Chem Lett; 2000 Oct 16; 10(20):2255-7. PubMed ID: 11055332.
    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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