Opioid receptors (ORs) are undisputed targets for the treatment of pain. Unfortunately, targeting these receptors therapeutically poses significant challenges including addiction, dependence, tolerance, and the appearance of side effects, such as respiratory depression and constipation. Moreover, misuse of prescription and illicit narcotics has resulted in the current opioid crisis. The mu-opioid receptor (MOR) is the cellular mediator of the effects of most commonly used opioids, and is a prototypical G protein-coupled receptor (GPCR) where new pharmacological, signalling and cell biology concepts have been coined. This review summarises the knowledge of the life cycle of this therapeutic target, including its biogenesis, trafficking to and from the plasma membrane, and how the regulation of these processes impacts its function and is related to pathophysiological conditions.

阿片受体（OR）是毫无争议的疼痛治疗靶标。不幸的是，针对这些受体的治疗带来了重大挑战，包括成瘾、依赖性、耐受性以及呼吸抑制和便秘等副作用的出现。此外，滥用处方药和非法麻醉品导致了当前的阿片类药物危机。 mu-阿片受体 (MOR) 是最常用阿片类药物作用的细胞介质，并且是一种典型的 G 蛋白偶联受体 (GPCR)，在其中创造了新的药理学、信号传导和细胞生物学概念。这篇综述总结了该治疗靶点生命周期的知识，包括其生物发生、进出质膜的运输，以及这些过程的调节如何影响其功能以及与病理生理条件的关系。