Uwaydah I M, May E L, Harris L S
J Med Chem. 1977 Nov;20(11):1374-7. doi: 10.1021/jm00221a004.
A series of N-substituted 9alpha-ethyl-2'-hydroxy-5-methyl-6,7-benzomorphans was synthesized and evaluated for their narcotic analgesic and antagonistic activities. Compounds 2a and 22 were as potent as morphine in the writhing (PPQ) and hot-plate tests, while a number of compounds demonstrated antagonistic activities greater than nalorphine. Generally, the compounds in this series show activities somewhat greater than the comparable compounds in the 5,9alpha-dimethyl-6,7-benzomorphan series for analgesic effect and similar or slightly less antagonistic potency.
合成了一系列N-取代的9α-乙基-2'-羟基-5-甲基-6,7-苯并吗啡烷，并对其麻醉镇痛和拮抗活性进行了评估。化合物2a和22在扭体（PPQ）和热板试验中的效力与吗啡相当，而一些化合物表现出比烯丙吗啡更强的拮抗活性。一般来说，该系列化合物在镇痛效果方面的活性略高于5,9α-二甲基-6,7-苯并吗啡烷系列中的类似化合物，拮抗效力相似或略低。
