Synthesis of a selective alpha-2A adrenoceptor antagonist, BRL 48962, and its characterization at cloned human alpha-adrenoceptors

被引：11
作者：
Beeley, LJ
Berge, JM
Chapman, H
Hieble, P
Kelly, J
Naselsky, DP
Rockell, CM
Young, PW
机构：
[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,EPSOM KT18 5XQ,SURREY,ENGLAND
[2] SMITHKLINE BEECHAM PHARMACEUT,DEPT VASC BIOL,WELWYN GARDEN CIT AL6 9AR,HERTS,ENGLAND
[3] SMITHKLINE BEECHAM PHARMACEUT,DEPT PHARMACOL,KING OF PRUSSIA,PA 19406
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 1995年 / 3卷 / 12期
关键词：
D O I：
10.1016/0968-0896(95)00157-3
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
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收藏
页码：1693 / 1698
页数：6
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