纳曲多尔
敌手
化学
类阿片
阿片受体
药理学
选择性
受体
阿片类拮抗剂
立体化学
内科学
生物化学
(+)-纳洛酮
医学
催化作用
作者
Helen Rogers,Ann G. Hayes,P.J. Birch,John R. Traynor,Andrew J. Lawrence
标识
DOI:10.1111/j.2042-7158.1990.tb05428.x
摘要
In the mouse vas deferens, naltrindole gave pKB values of 9.7, 8.3, and 7.5 at the delta-, mu-, and kappa-sites and in binding assays, pIC50 values of 9.6, 7.8 and 7.2 at the same sites. The affinity of naltrindole for the delta binding site was increased in the presence of sodium ions and 5'-guanylylimidophosphate. Naltrindole is, thus, a potent opioid antagonist with marked selectivity for the delta-opioid receptor.
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