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Forum on Immunopathological Diseases and Therapeutics
SJR: 0.309 SNIP: 0.041 CiteScore™: 0.18

ISSN Imprimer: 2151-8017
ISSN En ligne: 2151-8025

Archives: Volume 1, 2010 to Volume 7, 2016

Forum on Immunopathological Diseases and Therapeutics

DOI: 10.1615/ForumImmunDisTher.2012004796
pages 59-70

Molecular Mechanism of Opioid Analgesia

Christian Zollner
Department of Anesthesiology and Internal Medicine, University Hospital Hamburg-Eppendorf, Martinistr. 52, 20246 Hamburg Germany
Thomas Efferth
Department of Pharmaceutical Biology Institute of Pharmacy and Biochemistry Johannes Gutenberg University, Mainz, Germany

RÉSUMÉ

Opioids are still the most powerful drug in the treatment of acute and chronic pain. They comprise a class of drugs also known as narcotic analgesics. Opioid agonists can activate central and peripheral opioid receptors. Opioid receptors belong to the family of G protein−coupled receptors, which includes the typical structure of seven putative transmembrane (TM) regions. Opioid receptors are prototypical Gi/Go-coupled receptors because opioid signals are efficiently blocked by pertussis toxin, a bacterial toxin produced by Bordetella pertussis that ADP-ribosylates and inactivates the a subunits of Gi/Go proteins. The prolonged activation by opioids leads to the expression of compensating mechanisms in many neurons or neuronal systems. Soon after the discovery of opiate receptors it was reported that brain extracts contain a factor that inhibits acetylcholine release from nerves in the guinea pig ileum in a naloxone-reversible fashion, and that electrical stimulation of specific brain regions in rats elicited a profound analgesia, which was reversible by naloxone. After a century of effort, opioids remain the most effective treatment against pain. Most painkillers, such as aspirin, have an upper limit to their painkilling level, but opioids block more and more pain with increasing doses. Opioids are far from perfect, however; ongoing efforts by chemists and pharmacologists will continue to deliver new opioid drugs with higher potency and a reduction in severe side effects.


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