title: Pain-relieving prospects for adenosine receptors and ectonucleotidases.
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.
authors.affiliation: Department of Cell and Molecular Physiology, UNC Neuroscience Center, University of North Carolina, Chapel Hill, NC 27599, USA. zylka@med.unc.edu
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Zylka
mesh_terms: D015720:5'-Nucleotidase / Q000627:therapeutic use*; D000135:Acid Phosphatase; D015670:Acupuncture Therapy; D000241:Adenosine / Q000378:metabolism; D000249:Adenosine Monophosphate / Q000378:metabolism; D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D006801:Humans; D006930:Hyperalgesia / Q000188:drug therapy / Q000378:metabolism; D007249:Inflammation / Q000188:drug therapy; D009437:Neuralgia / Q000188:drug therapy*; D009619:Nociceptors / Q000187:drug effects; D017027:Protein Tyrosine Phosphatases / Q000627:therapeutic use; D058906:Purinergic P1 Receptor Agonists / Q000627:therapeutic use*; D018047:Receptors, Purinergic P1 / Q000187:drug effects*; D011994:Recombinant Proteins / Q000627:therapeutic use
chemical_list: D000700:Analgesics; D058906:Purinergic P1 Receptor Agonists; D018047:Receptors, Purinergic P1; D011994:Recombinant Proteins; D000249:Adenosine Monophosphate; D000135:Acid Phosphatase; C428439:prostatic acid phosphatase; D017027:Protein Tyrosine Phosphatases; D015720:5'-Nucleotidase; D000241:Adenosine