Zádor Ferenc, Király Kornél, Essmat Nariman, Al-Khrasani Mahmoud
Department of Pharmacology and Pharmacotherapy, Faculty of Medicine, Semmelweis University, Budapest, Hungary.
Front Mol Biosci. 2022 Jun 13;9:900547. doi: 10.3389/fmolb.2022.900547. eCollection 2022.
Opioid agonists produce their analgesic effects primarily by acting at the µ-opioid receptor (µOR). µOR agonists with different efficacies exert diverse molecular changes in the µOR which dictate the faith of the receptor's signaling pathway and possibly it's the degree of desensitization. Since the development of the active conformations of the µOR, growing data have been published in relation to ligand-specific changes in µOR activation. In this regard, this review summarizes recent data regarding the most studied opioid agonists in µOR activation, including how these ligands are recognized by the µOR, how their binding signal is transmitted toward the intracellular parts of the µOR, and finally, what type of large-scale movements do these changes trigger in the µOR's domains.
阿片类激动剂主要通过作用于μ-阿片受体（μOR）产生镇痛作用。具有不同效力的μOR激动剂会在μOR中引发不同的分子变化，这些变化决定了受体信号通路的走向以及可能的脱敏程度。自从μOR的活性构象被发现以来，关于μOR激活中配体特异性变化的相关数据不断涌现。在这方面，本综述总结了有关μOR激活中研究最多的阿片类激动剂的最新数据，包括这些配体如何被μOR识别，它们的结合信号如何向μOR的细胞内部分传递，以及最后，这些变化在μOR结构域中引发了何种类型的大规模运动。
