期刊
JOURNAL OF BIOLOGICAL CHEMISTRY
卷 286, 期 33, 页码 28723-28728出版社
AMER SOC BIOCHEMISTRY MOLECULAR BIOLOGY INC
DOI: 10.1074/jbc.M110.202853
关键词
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资金
- National Institute on Drug Abuse [DA026430]
- National Institutes of Health United States Public Health Service from NIGMS [2T32 GM007270]
- Spanish Ministerio de Ciencia e Innovacion (MICINN)
- European Social Fund [SAF2010-22198-C02-01]
- Ramon y Cajal Program
Agonists at cannabinoid receptors, such as the phytocannabinoid Delta(9)-tetrahydrocannabinol, exert a remarkable array of therapeutic effects but are also associated with undesirable psychoactive side effects. Conversely, targeting enzymes that hydrolyze endocannabinoids (eCBs) allows for more precise fine-tuning of cannabinoid receptor signaling, thus providing therapeutic relief with reduced side effects. Here, we report the development and characterization of an inhibitor of eCB hydrolysis, UCM710, which augments both N-arachidonoylethanolamine and 2-arachidonoylglycerol levels in neurons. This compound displays a unique pharmacological profile in that it inhibits fatty acid amide hydrolase and alpha/beta-hydrolase domain 6 but not monoacylglycerol lipase. Thus, UCM710 represents a novel tool to delineate the therapeutic potential of compounds that manipulate a subset of enzymes that control eCB signaling.
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