Opioid peptides and opiates differ in receptor selectivity
Opioid peptides and opiates differ in receptor selectivity
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阿片肽和阿片制剂的受体选择性不同
DOI：
10.1016/0306-4530(77)90031-2
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发表时间：
1977
影响因子：
3.7
通讯作者：
L. Terenius
中科院分区：
文献类型：
--
作者：
L. Terenius
(1)本文以氚标记的二氢吗啡、纳洛酮和亮脑啡肽为放射性指示剂，以各种阿片肽和阿片类药物为竞争剂，研究了大鼠全脑阿片受体的结合特性。(2)二氢吗啡显示出与被各种阿片激动剂和拮抗剂竞争性阻断的位点（DHM位点）的高亲和力结合。(3)纳洛酮与其他位点结合，这些位点也与其他麻醉剂拮抗剂（NAL位点）强结合。(4)拟吗啡脑啡肽对DHM位点有较高的选择性，而促肾上腺皮质激素片段和生长抑素的选择性较低。(5)亮氨酸脑啡肽似乎结合到不同的网站（EKN网站）与DHM网站类似的亲和力。(6)二氢吗啡和纳洛酮对DHM位点的亲和力高于对EKN位点的亲和力。(7)总之，至少可以观察到三种阿片结合位点。受体群体的这些差异可能与功能差异有关。
(1) The binding properties of opioid receptors in whole rat cerebrum have been studied with tritium-labelled dihydromorphine, naltrexone and Leu-enkephalin as radioindicators and various opioid peptides and opiates as competitors. (2) Dihydromorphine shows high affinity binding to sites which are competitively blocked by various opiate agonists and antagonists (DHM sites). (3) Naltrexone binds to additional sites which also strongly bind other narcotic antagonists (NAL sites). (4) The morphinomimetic enkephalins show high selectivity for DHM sites while ACTH fragments and somatostatin show less selectivity. (5) Leu-enkephalin appears to bind to separate sites (EKN sites) with similar affinity to that for DHM sites. (6) Both dihydromorphine and naltrexone show higher affinity for DHM sites than for EKN sites. (7) In conclusion, at least three kinds of opioid binding sites are observable. These differences in receptor populations may relate to functional differences.