选择性α-2A肾上腺素能受体拮抗剂BRL 48962的合成及其在克隆的人α-肾上腺素能受体上的特性研究
Synthesis of a selective alpha-2A adrenoceptor antagonist, BRL 48962, and its characterization at cloned human alpha-adrenoceptors.
作者信息
Beeley L J, Berge J M, Chapman H, Hieble P, Kelly J, Naselsky D P, Rockell C M, Young P W
机构信息
Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, Great Burgh, Epsom, Surrey, U.K.
出版信息
Bioorg Med Chem. 1995 Dec;3(12):1693-8. doi: 10.1016/0968-0896(95)00157-3.
PMID:8770394
Abstract
The chiral synthesis of the potent and selective alpha-2A antagonist, BRL 48962, is described. Evaluation of BRL 48962 at cloned human alpha-adrenoceptors indicates that this antagonist has a selectivity in the order of 30-fold for the alpha-2A subtype.
摘要
描述了强效和选择性α-2A拮抗剂BRL 48962的手性合成。在克隆的人α-肾上腺素能受体上对BRL 48962进行评估表明，该拮抗剂对α-2A亚型的选择性约为30倍。
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