5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone: a long-lasting mu-opioid receptor antagonist devoid of agonist properties.
5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone: a long-lasting mu-opioid receptor antagonist devoid of agonist properties.
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5 beta-Mmethyl-14 beta-(p-硝基肉桂酰氨基)-7,8-二氢吗啡酮：一种长效 mu-阿片受体拮抗剂，缺乏激动剂特性。
DOI：
10.1016/0014-2999(93)90423-f
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发表时间：
1993
影响因子：
5
通讯作者：
Bidlack,JM
中科院分区：
文献类型：
--
作者：
Jiang,Q;Sebastian,A;Archer,S;Bidlack,JM
5β-甲基-14β-（对硝基氨基）-7,8-二氢吗啡酮（et - camo）在试验前8 ~ 72 h单次灌胃1 nmol后可抑制吗啡诱导的抗痫性，但对δ-或κ-阿片受体介导的抗痫性无影响。在小鼠摇尾试验中，MET-CAMO在高达100 nmol的剂量下没有激动作用。MET-CAMO是第一个n -甲基化吗啡衍生物，具有持久的μ选择性阿片受体拮抗作用，但没有激动性。
5β-Methyl-14β-(p-nitrocinnamoylamino)-7,8-dihydromorphinone (MET-CAMO) suppressed morphine-induced antinociception but had no effect on antinociception mediated by δ-or κ-opioid receptors after a single i.c.v. 1-nmol injection from 8 to 72 h before testing. MET-CAMO had no agonist effects in the mouse tail-flick assay in doses up to 100 nmol. MET-CAMO is the first N-methylated morphine derivative which shows such long-lasting μ-selective opioid receptor antagonism with no agonistic properties.