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Trends Mol Med. 2011 Apr;17(4):188-96. doi: 10.1016/j.molmed.2010.12.006. Epub 2011 Jan 13.

Pain-relieving prospects for adenosine receptors and ectonucleotidases.

Author information

1
Department of Cell and Molecular Physiology, UNC Neuroscience Center, University of North Carolina, Chapel Hill, NC 27599, USA. zylka@med.unc.edu

Abstract

Adenosine receptor agonists have potent antinociceptive effects in diverse preclinical models of chronic pain. By contrast, the efficacy of adenosine and adenosine receptor agonists in treating pain in humans is unclear. Two ectonucleotidases that generate adenosine in nociceptive neurons were recently identified. When injected spinally, these enzymes have long-lasting adenosine A(1) receptor-dependent antinociceptive effects in inflammatory and neuropathic pain models. Furthermore, recent findings indicate that spinal adenosine A(2A) receptor activation can enduringly inhibit neuropathic pain symptoms. Collectively, these studies suggest the possibility of treating chronic pain in humans by targeting specific adenosine receptor subtypes in anatomically defined regions with agonists or with ectonucleotidases that generate adenosine.

PMID:
21236731
PMCID:
PMC3078941
DOI:
10.1016/j.molmed.2010.12.006
[Indexed for MEDLINE]
Free PMC Article
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