二苯基亚砜作为毒蕈碱M2受体的选择性拮抗剂。
Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
作者信息
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
机构信息
Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.
出版信息
Bioorg Med Chem Lett. 2000 Oct 16;10(20):2255-7. doi: 10.1016/s0960-894x(00)00438-8.
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.
摘要
对[4-(苯磺酰基)苯基]甲基哌嗪的构效关系研究导致发现了4-环己基-α-[4-[[4-甲氧基苯基(S)-亚磺酰基]苯基]-1-哌嗪乙腈，1，一种M2选择性毒蕈碱拮抗剂。对克隆的人M2受体的亲和力为2.7 nM；M1/M2选择性为40倍。
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