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Inhibitors of monoacylglycerol lipase as novel analgesics
Author(s) -
Hohmann A G
Publication year - 2007
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0707153
Subject(s) - monoacylglycerol lipase , endocannabinoid system , cannabinoid receptor , 2 arachidonoylglycerol , pharmacology , cannabinoid , analgesic , nociception , diacylglycerol lipase , peripheral , chemistry , receptor , lipase , medicine , enzyme , biochemistry , agonist
2‐Arachidonoylglycerol (2‐AG) is an endogenous cannabinoid (endocannabinoid) lipid whose functions remain poorly understood. Guindon and colleagues report the novel finding that exogenous application of 2‐AG induces peripheral antinociceptive effects that are mediated, at least in part, by actions at peripheral cannabinoid CB 2 receptors. URB602, a recently described inhibitor of monoacylglycerol lipase, an enzyme that catalyzes 2‐AG hydrolysis in vivo , also induced peripheral antinociceptive effects and enhanced the actions of 2‐AG. Peripheral analgesic mechanisms represent promising therapeutic targets for suppressing pain in the absence of unwanted central nervous system side‐effects (e.g. psychoactivity) associated with activation of central CB 1 receptors. The therapeutic potential of inhibitors of 2‐AG deactivation for the treatment of inflammatory pain is discussed. British Journal of Pharmacology (2007) 150 , 673–675. doi: 10.1038/sj.bjp.0707153