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Modulation of opioid analgesia, tolerance and dependence by Gs-coupled, GM1 ganglioside-regulated opioid receptor

S M Crain1, K F Shen

  • 1Department of Neuroscience, Albert Einstein College of Medicine, Yeshiva University, Bronx, NY 10461, USA.

Trends in Pharmacological Sciences
|October 24, 1998
PubMed

Insights

This study highlights the crucial role of GM1 ganglioside in modulating opioid receptor functions, impacting pain relief, tolerance, and dependence. Understanding GM1 levels is key to exploring opioid efficacy.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Glycobiology

Background:

  • Opioid agonists directly excite neurons, a finding confirmed across many labs.
  • Recent reviews on opioid stimulatory mechanisms have overlooked the role of GM1 ganglioside.

Purpose of the Study:

  • To address the critical role of endogenous GM1 ganglioside in regulating Gs-coupled, excitatory opioid receptor functions.
  • To explore the influence of GM1 concentration on opioid receptor-mediated analgesia, tolerance, and dependence.

Main Methods:

  • Review of existing literature on opioid receptor function and GM1 ganglioside.
  • Analysis of evidence linking GM1 concentration to opioid effects.

Main Results:

  • Evidence suggests GM1 ganglioside concentration significantly modulates opioid receptor-mediated analgesia.
  • GM1 levels appear to play a role in the development of opioid tolerance and dependence.

Conclusions:

  • GM1 ganglioside is a critical factor in modulating excitatory opioid receptor functions.
  • Neuronal GM1 concentration is a key determinant of opioid efficacy and side effects, including analgesia, tolerance, and dependence.

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