Zhang Yan, Xiong Wei, Lin Xiaojing, Ma Xiang, Yu Long-Chuan
Laboratory of Neurobiology, College of Life Sciences, Peking University, Beijing 100871, China.
Neurosci Biobehav Rev. 2009 Sep;33(8):1192-7. doi: 10.1016/j.neubiorev.2009.03.007. Epub 2009 Mar 20.
Opiates, including morphine, are widely used drugs for antinociception in clinics. Prolonged treatments of opioids induce both tolerance and dependence, which are the major side effects of opioid therapy. One of the mechanisms for the development of tolerance and dependence is implicated to be opioid-receptor trafficking. Here we review the current understandings of opioid-receptor phosphorylation, endocytosis and desensitization after repeated agonist treatments. Also, the role of G-protein coupled receptor kinases in opioid-receptor phosphorylation is discussed. How to associate these observations to physiological and behavioral changes in animal models and clinics is still under investigation.
阿片类药物，包括吗啡，是临床上广泛用于镇痛的药物。长期使用阿片类药物会导致耐受性和依赖性，这是阿片类药物治疗的主要副作用。耐受性和依赖性产生的机制之一被认为与阿片受体的转运有关。在此，我们综述了反复给予激动剂后阿片受体磷酸化、内吞作用和脱敏作用的当前认识。此外，还讨论了G蛋白偶联受体激酶在阿片受体磷酸化中的作用。如何将这些观察结果与动物模型和临床中的生理及行为变化联系起来仍在研究中。
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