9-羟基化对苯并吗啡烷拮抗剂活性的影响。
Effect of 9-hydroxylation on benzomorphan antagonist activity.
作者信息
Albertson N F
出版信息
J Med Chem. 1975 Jun;18(6):619-21. doi: 10.1021/jm00240a019.
PMID:1151978
Abstract
In a benzomorphan bearing an antagonist side chain, introduction on the methano bridge of a hydroxyl oriented away from nitrogen has little effect on antagonist activity whereas a hydroxyl oriented toward nitrogen enhances this activity. Hydroxylation tends to decrease analgesic activity.
摘要
在带有拮抗剂侧链的苯并吗啡烷中，在远离氮原子的甲撑桥上引入羟基对拮抗剂活性影响很小，而朝向氮原子的羟基则会增强这种活性。羟基化往往会降低镇痛活性。
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