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药物辨别研究。

Drug discrimination studies.

作者信息

Holtzman S G

出版信息

Drug Alcohol Depend. 1985 Feb;14(3-4):263-82. doi: 10.1016/0376-8716(85)90061-4.

Abstract

Opioid agonists and agonist/antagonists comprise a heterogeneous body of compounds that can be partitioned into at least three groups on the basis of their discriminative stimulus properties in several animal species: (1) stimulus effects similar to those of morphine or fentanyl and blocked completely by low doses of antagonists, such as naloxone and naltrexone; (2) stimulus effects similar to those of ethylketocyclazocine or nalorphine and blocked by higher doses of antagonists; (3) stimulus effects similar to those N-allylnormetazocine or phencyclidine and not blocked by antagonists. This diversity of stimulus properties is consistent with other evidence that multiple populations of receptors mediate the actions of opioids. In man, drugs in group 1 produce subjective effects that are entirely morphine-like and highly reinforcing whereas drugs in groups 2 and 3 produce dysphoric and psychotomimetic subjective effects. Thus, discriminative stimulus properties of opioids appear to reflect drug actions at the neuronal level that are directly relevant to potential for abuse in man.

摘要

阿片类激动剂和激动剂/拮抗剂由多种化合物组成,根据它们在几种动物物种中的辨别刺激特性,可将其至少分为三组:(1)刺激效应类似于吗啡或芬太尼,可被低剂量拮抗剂(如纳洛酮和纳曲酮)完全阻断;(2)刺激效应类似于乙基酮环唑辛或烯丙吗啡,可被高剂量拮抗剂阻断;(3)刺激效应类似于N-烯丙基去甲左啡诺或苯环己哌啶,且不被拮抗剂阻断。这种刺激特性的多样性与其他证据一致,即多种受体群体介导阿片类药物的作用。在人类中,第1组药物产生的主观效应完全类似于吗啡,且具有高度强化作用,而第2组和第3组药物产生烦躁不安和拟精神病性的主观效应。因此,阿片类药物的辨别刺激特性似乎反映了其在神经元水平上与人类滥用潜力直接相关的药物作用。

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