Receptor trafficking induced by mu-opioid-receptor phosphorylation.
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.
Zhang
Yan
Y
Laboratory of Neurobiology, College of Life Sciences, Peking University, Beijing 100871, China. yanzhang@pku.edu.cn
Xiong
Wei
W
Lin
Xiaojing
X
Ma
Xiang
X
Yu
Long-Chuan
LC
D000818:Animals; D004705:Endocytosis / Q000502:physiology*; D054768:G-Protein-Coupled Receptor Kinases / Q000378:metabolism*; D006801:Humans; D010766:Phosphorylation; D021381:Protein Transport; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000378:metabolism*; D015290:Second Messenger Systems / Q000502:physiology; D015398:Signal Transduction / Q000502:physiology*
D017450:Receptors, Opioid, mu; D054768:G-Protein-Coupled Receptor Kinases