Massotte D, Kieffer B L
Département des récepteurs et protéines membranaires, (CNRS UPR 9050), Ecole Supérieure de Biotechnologie de Strasbourg, Illkirch-Graffenstaden, France.
Essays Biochem. 1998;33:65-77. doi: 10.1042/bse0330065.
Opioid receptors mediate the strong analgesic and addictive actions of exogenous opiates, the prototype of which is morphine. The opioid system consists of a family of endogenous opioid peptides and three receptor types, m, d and k. It is widely distributed throughout the CNS and regulates a large diversity of physiological functions, including pain perception and mood control. The recent cloning of opioid receptors has opened up a new era in opioid research. The molecular basis of opioid action may now be addressed by in vitro structure-function studies of recombinant receptors and by in vivo gene targeting. Novel drug design strategies based on data obtained from molecular approaches will be developed in order to generate the long-sought non-addictive analgesic.
阿片受体介导外源性阿片类药物的强效镇痛和成瘾作用，其原型为吗啡。阿片系统由一族内源性阿片肽和三种受体类型（μ、δ和κ）组成。它广泛分布于中枢神经系统，并调节多种生理功能，包括痛觉感知和情绪控制。最近阿片受体的克隆开启了阿片研究的新纪元。现在可以通过重组受体的体外结构-功能研究和体内基因靶向研究来探讨阿片作用的分子基础。基于从分子方法获得的数据，将开发新的药物设计策略，以产生长期以来寻求的非成瘾性镇痛药。
