麻醉拮抗剂。某些取代的1,2,3,4,5,6-六氢-1,4:2,6-二亚甲基-3-苯并氮杂卓的合成与评价。
Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
作者信息
Montzka T A, Matiskella J D
出版信息
J Med Chem. 1977 Mar;20(3):453-6. doi: 10.1021/jm00213a027.
PMID:845878
Abstract
A seres of (+/-)-N-substituted 6-ethyl-or -methyl-8-hydroxy-1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines has been prepared from 6 hydroxytropinone. The N-cyclopropylmethyl compounds 10a and 10b were found to be strong narcotic antagonists approximately equivalent to nalorphine. Only slight analgetic activity was found in any of these compounds including the two N-methyl analogues.
摘要
已从6-羟基托品酮制备了一系列（±）-N-取代的6-乙基或-甲基-8-羟基-1,2,3,4,5,6-六氢-1,4:2,6-二亚甲基-3-苯并氮杂环辛烷。发现N-环丙基甲基化合物10a和10b是强效麻醉拮抗剂，效力约与烯丙吗啡相当。在这些化合物中，包括两种N-甲基类似物，均未发现明显的镇痛活性。
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