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Frontiers in pharmacology · Jan 2014
ReviewOpioid receptor desensitization: mechanisms and its link to tolerance.
- Stéphane Allouche, Florence Noble, and Nicolas Marie.
- Laboratoire de Signalisation, Électrophysiologie et Imagerie des Lésions D'ischémie-Reperfusion Myocardique, Université de Caen, UPRES EA 4650, IFR 146 ICORE Caen, France.
- Front Pharmacol. 2014 Jan 1; 5: 280.
AbstractOpioid receptors (OR) are part of the class A of G-protein coupled receptors and the target of the opiates, the most powerful analgesic molecules used in clinic. During a protracted use, a tolerance to analgesic effect develops resulting in a reduction of the effectiveness. So understanding mechanisms of tolerance is a great challenge and may help to find new strategies to tackle this side effect. This review will summarize receptor-related mechanisms that could underlie tolerance especially receptor desensitization. We will focus on the latest data obtained on molecular mechanisms involved in opioid receptor desensitization: phosphorylation, receptor uncoupling, internalization, and post-endocytic fate of the receptor.
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