Endocytosis of μ opioid receptors inhibits morphine tolerance

Abstract

Abstract: Opioids are the most effective analgesics. However, prolonged administration of morphine, the representative of opioids, results in tolerance, limiting the therapeutic utility of opiate drugs. Studies have recently suggested that endocytosis of μ opioid receptors attenuates opioid tolerance. The ability of inducing endocytosis of opioid receptor is agonist-dependent. It has been shown that the endocytotic efficacy of opioids are negatively correlated with opioid tolerance. Receptor internalization reduced adaptive changes in signaling pathways that are involved in the development of opioid tolerance. Moreover, endocytosised μ-opioid receptors are rapidly recycled back to the cell membrane surface resuming their normal function. Therefore, tolerance does not occur. Thus, the study of receptor endocytosis and trafficking following the activation of the receptors can help the therapy for chronic pain.

Key words: μ opioid receptors;, Morphine tolerance, Receptor internalization, G protein signaling pathways

CLC Number:

R388
Q42

LV Qing-qin, CHEN Ting-jun, HONG Yan-guo. Endocytosis of μ opioid receptors inhibits morphine tolerance[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(10): 1185-1190.

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