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B/C-顺式和反式-1,3,4,9,10,10a-六氢-2H-10,4a-亚甲基亚氨基乙菲(高和高异吗啡喃)衍生物作为镇痛药。

B/C-cis- and -trans-1,3,4,9,10,10a-Hexahydro-2H-10,4a-methanoiminoethanophenanthrene (homo- and homoisomorphinan) derivatives as analgesics.

作者信息

Shiotani S, Kometani T

出版信息

J Med Chem. 1977 Jul;20(7):976-8. doi: 10.1021/jm00217a027.

Abstract

N-Alkyl derivatives of B/C-cis- and B/C-trans-6-hydroxy-1,3,4,9,10,10a-hexahydro-2H-10,4a-methanoimino-ethanophenanthrene have been prepared. The analgesic potency and physical dependence capacity of these compounds were determined. The N-methyl derivatives were analgesically equipotent with morphine. None of these compounds except the N-methyl-B/C-trans isomer 2b suppressed or precipitated the abstinence syndrome. Compound 2b was a narcotic agonist. The N-methyl-B/C-cis compound 2a appears to warrant further examination for its potential as a potent analgesic having no physical dependence liability.

摘要

已制备了B/C-顺式和B/C-反式-6-羟基-1,3,4,9,10,10a-六氢-2H-10,4a-亚甲基亚氨基-乙菲的N-烷基衍生物。测定了这些化合物的镇痛效力和身体依赖性能力。N-甲基衍生物在镇痛方面与吗啡等效。除N-甲基-B/C-反式异构体2b外,这些化合物均未抑制或引发戒断综合征。化合物2b是一种麻醉激动剂。N-甲基-B/C-顺式化合物2a因其作为一种无身体依赖性风险的强效镇痛药的潜力而似乎值得进一步研究。

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