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Updated: Apr 18, 2026

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
Published on: July 29, 2014
Opioid receptor desensitization: mechanisms and its link to tolerance
Stéphane Allouche1, Florence Noble2, Nicolas Marie2
1Laboratoire de Signalisation, Électrophysiologie et Imagerie des Lésions D'ischémie-Reperfusion Myocardique, Université de Caen, UPRES EA 4650, IFR 146 ICORE Caen, France.
Abstract:
Opioid 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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