阿片受体：一种解释阿片激动剂和拮抗剂构效关系的模型。
The opiate receptor: a model explaining structure-activity relationships of opiate agonists and antagonists.
作者信息
Feinberg A P, Creese I, Snyder S H
出版信息
Proc Natl Acad Sci U S A. 1976 Nov;73(11):4215-9. doi: 10.1073/pnas.73.11.4215.
Abstract
A model of the opiate receptor is proposed which explains structure-activity relationships of opiate drugs, including (i) the unique potency of certain opiates such as etonitazene, fentanyl, phenazocine, and oripavines; (ii) the role of N-allyl substituents in conferring antagonist properties; and (iii) chemical features that afford "pure" antagonists. The model indicates mlecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.
摘要
提出了一种阿片受体模型，该模型解释了阿片类药物的构效关系，包括：（i）某些阿片类药物如依托尼秦、芬太尼、非那佐辛和阿片碱的独特效力；（ii）N-烯丙基取代基在赋予拮抗剂特性方面的作用；以及（iii）产生“纯”拮抗剂的化学特征。该模型指出了阿片受体在以高亲和力结合激动剂或拮抗剂的各自状态之间相互转化的分子机制。
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