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14-Amino-4,5-epoxymorphinan derivatives and their pharmacological actions.
Topics in Current Chemistry ( IF 7.1 ) Pub Date : 2011-06-02 , DOI: 10.1007/128_2010_89
John W Lewis 1 , Stephen M Husbands
Affiliation  

14-Hydroxy-7,8-dihydromorphinone (oxymorphone) and its derivatives (oxycodone, naloxone, naltrexone) have become among the most important clinical agents to have been produced from opium. 14-Aminocodeinone and its 7,8-dihydro and morphinone derivatives are of more recent origin thanks to the work of Professor Gordon Kirby and his collaborators. The 14-amino parent compounds have proved of limited interest but their 14-acylamino- and 14-alkylamino derivatives have been extensively studied. The 4'-substituted cinnamoylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones, C-CAM and M-CAM are the best available selective MOR irreversible antagonists and the related dihydrocodeinone MC-CAM, 4'-chloro-cinnamoylamino-17-cyclopropylmethyl-7,8-dihydronorcodeinone, is a long-acting MOR partial agonist with extended MOR-pseudoirreversible antagonist activity that could be a candidate for pharmacotherapy of opiate abuse/dependence.

中文翻译:

14-氨基-4,5-环氧吗啡喃衍生物及其药理作用。

14-羟基-7,8-二氢吗啡酮(羟吗啡酮)及其衍生物(羟考酮,纳洛酮,纳曲酮)已成为鸦片生产中最重要的临床药物。由于戈登·柯比教授和他的合作者的工作,14-氨基可待因酮及其7,8-二氢和吗啡酮衍生物的起源更近。已经证明了14-氨基母体化合物的兴趣有限,但是已经广泛研究了它们的14-酰基氨基-和14-烷基氨基衍生物。4'-取代的肉桂酰氨基-17-环丙基甲基7,8-二氢去甲吗啡酮,C-CAM和M-CAM是可获得的最佳MOR不可逆拮抗剂,以及相关的二氢可待因酮MC-CAM,4'-氯-肉桂酰氨基17-环丙基甲基-7,8-二氢去甲可待因酮,
更新日期:2019-11-01
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