Affinity labels for opioid receptors.
Affinity labels for opioid receptors.
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DOI：
10.1146/annurev.pa.25.040185.001205
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发表时间：
1985
影响因子：
12.5
通讯作者：
A. Takemori;P. Portoghese
中科院分区：
文献类型：
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作者：
A. Takemori;P. Portoghese
多种阿片受体以及与单一受体相互作用的多种模式的概念源自两个趋同的研究方向。该提议最初基于对镇痛配体之间广泛的结构-活性关系的详细分析 (1, 2)。很快，药理学研究补充了这一概念并提供了更详细的框架 (3-5)。最近，通过许多体外和体内生物测定以及阿片受体结合测定，多受体概念得到了推进。许多评论总结了此类研究的数据 (6-13)。基于对慢性脊柱犬进行的广泛药理学测试，Martin 和同事 (14, 15) 建议将那些受体命名为 1-'-、K 或 IT，假定吗啡、酮他佐辛和 SKF 10,047（N-烯丙基去甲佐辛）分别在这些受体上相互作用。通过使用体外 (17-19) 和体内 (5) 的 pA2 概念 (16) 以及各种其他体内测试方法 (20-22)，强化了吗啡样和酮佐辛或纳洛啡样化合物的不同受体的概念。脑啡肽和 l3-内啡肽分别通过 8 和 E 受体介导其作用，已在体外得到鉴定 (19,23,24)。体内 Thea 受体与许多生理功能有关
The concept of multiple opioid receptors and multiple modes of interaction with a single receptor emanated from two convergent lines of research. This proposal was based originally on a detailed analysis of a wide spectrum of structure-activity relationships among analgesic ligands (1, 2). Very soon, pharmacological studies complemented and provided a more detailed framework for this concept (3-5). More recently, the multiple receptor concept has been advanced through a number of in vitro and in vivo biological assays and the opioid receptor binding assay. Data from such studies have been summarized in a number of reviews (6-13). Based on a wide range of pharmacological tests in the chronic spinal dog, Martin and coworkers (14, 15) suggested the designation 1-'-, K, or IT for those receptors at which morphine, ketazocine, and SKF 10,047 (N-allyl normetazocine) respectively are postulated to interact. The notion of different receptors for morphine-like and ketazocineor nalorphine-like compounds has been strengthened by the use of the pA2 concept (16) both in vitro (17-19) and in vivo (5) and by various other testing methods in vivo (20-22). The 8 and E receptor through which the enkephalins and l3-endorphin respectively are thought to mediate their effects have been identified in vitro (19,23,24). Thea receptor in vivo has been implicated in a number of physiological functions