Frontiers in Pharmacology (Dec 2014)

Opioid receptor desensitization: mechanisms and its link to tolerance

  • Stéphane eAllouche,
  • Florence eNoble,
  • Florence eNoble,
  • Florence eNoble,
  • Nicolas eMarie,
  • Nicolas eMarie,
  • Nicolas eMarie

DOI
https://doi.org/10.3389/fphar.2014.00280
Journal volume & issue
Vol. 5

Abstract

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Opioid receptors 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.

Keywords