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Pharmacol Ther. 2008 Jan;117(1):141-61. Epub 2007 Sep 22.

Modulation of pain transmission by G-protein-coupled receptors.

Author information

1
Department of Anesthesiology and Pain Medicine, The University of Texas M.D. Anderson Cancer Center, Program in Neuroscience, The University of Texas Graduate School of Biomedical Sciences, Houston, TX 77225, United States. huilinpan@mdanderson.org

Abstract

The heterotrimeric G-protein-coupled receptors (GPCR) represent the largest and most diverse family of cell surface receptors and proteins. GPCR are widely distributed in the peripheral and central nervous systems and are one of the most important therapeutic targets in pain medicine. GPCR are present on the plasma membrane of neurons and their terminals along the nociceptive pathways and are closely associated with the modulation of pain transmission. GPCR that can produce analgesia upon activation include opioid, cannabinoid, alpha2-adrenergic, muscarinic acetylcholine, gamma-aminobutyric acidB (GABAB), groups II and III metabotropic glutamate, and somatostatin receptors. Recent studies have led to a better understanding of the role of these GPCR in the regulation of pain transmission. Here, we review the current knowledge about the cellular and molecular mechanisms that underlie the analgesic actions of GPCR agonists, with a focus on their effects on ion channels expressed on nociceptive sensory neurons and on synaptic transmission at the spinal cord level.

PMID:
17959251
PMCID:
PMC2965406
DOI:
10.1016/j.pharmthera.2007.09.003
[Indexed for MEDLINE]
Free PMC Article
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