Kosterlitz H W
Unit for Research on Addictive Drugs, University of Aberdeen, Marischal College, U.K.
Pol J Pharmacol Pharm. 1987 Sep-Oct;39(5):571-6.
Since the endogenous opioid peptides bind to more than one of the types of binding sites, it is important to have synthetic compounds that bind almost exclusively at one site. There are now such agonists available but antagonists are still required that interact exclusively with one opioid site. The results obtained with opioid peptides or non-peptides having such qualities will be the physiological basis for a correlation of the binding at mu-, delta- and kappa-receptors with their pharmacological effects. It is important to realize that almost all endogenous opioid ligands are degraded by peptidases and that it is necessary to have synthetic non-toxic inhibitors of those peptidases that play a role in opioid transmission. Related to this problem is the need to develop methods for the study of the release of various endogenous opioid peptides under physiological conditions.
由于内源性阿片肽可与多种类型的结合位点结合，因此拥有几乎只在一个位点结合的合成化合物很重要。目前已有这类激动剂，但仍需要能专门与一个阿片样物质位点相互作用的拮抗剂。用具有此类特性的阿片肽或非肽所获得的结果，将成为μ-、δ-和κ-受体结合与其药理作用相关性的生理学基础。必须认识到，几乎所有内源性阿片样物质配体都会被肽酶降解，因此有必要合成无毒的肽酶抑制剂，这些肽酶在阿片样物质传递中起作用。与此问题相关的是，需要开发在生理条件下研究各种内源性阿片肽释放的方法。
