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In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML 29: antinociceptive activity without cannabimimetic side effects
Author(s) -
IgnatowskaJankowska B M,
Ghosh S,
Crowe M S,
Kinsey S G,
Niphakis M J,
Abdullah R A,
Tao Q,
O' Neal S T,
Walentiny D M,
Wiley J L,
Cravatt B F,
Lichtman A H
Publication year - 2014
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 - 10.1111/bph.12298
Subject(s) - monoacylglycerol lipase , anandamide , catalepsy , pharmacology , chemistry , fatty acid amide hydrolase , cannabinoid , endocannabinoid system , cannabinoid receptor , hyperalgesia , allodynia , diacylglycerol lipase , agonist , nociception , receptor , biochemistry , medicine , endocrinology , dopamine , haloperidol
Since monoacylglycerol lipase (MAGL) has been firmly established as the predominant catabolic enzyme of the endocannabinoid 2-arachidonoylglycerol (2-AG), a great need has emerged for the development of highly selective MAGL inhibitors. Here, we tested the in vivo effects of one such compound, KML29 (1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate).