Osei-Gyimah P, Archer S, Gillan M G, Kosterlitz H W
J Med Chem. 1981 Feb;24(2):212-4. doi: 10.1021/jm00134a018.
A series of N-(cyclopropylmethyl)-14 beta-substituted-normorphine analogues was synthesized and tested for opioid agonist and antagonist activity in the guinea pig ileum and mouse vas deferens preparations. The 14 beta-bromo compound proved to be a pure antagonist equal in potency to naloxone in the guinea pig ileum assay. In contrast to N-(cyclopropylmethyl)-14 beta-hydroxynormorphine which was a pure antagonist, the corresponding sulfur analogue was about equal to nalorphine in agonist and antagonist potency.
合成了一系列N-（环丙基甲基）-14β-取代去甲吗啡类似物，并在豚鼠回肠和小鼠输精管制备物中测试其阿片样物质激动剂和拮抗剂活性。在豚鼠回肠试验中，14β-溴化合物被证明是一种纯拮抗剂，其效力与纳洛酮相当。与纯拮抗剂N-（环丙基甲基）-14β-羟基去甲吗啡相反，相应的硫类似物在激动剂和拮抗剂效力方面约与纳洛芬相当。
