| Title : Dual inhibition of alpha\/beta-hydrolase domain 6 and fatty acid amide hydrolase increases endocannabinoid levels in neurons - Marrs_2011_J.Biol.Chem_286_28723 |
| Author(s) : Marrs WR , Horne EA , Ortega-Gutierrez S , Cisneros JA , Xu C , Lin YH , Muccioli GG , Lopez-Rodriguez ML , Stella N |
| Ref : Journal of Biological Chemistry , 286 :28723 , 2011 |
| Abstract : 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. |
| ESTHER : Marrs_2011_J.Biol.Chem_286_28723 |
| PubMedSearch : Marrs_2011_J.Biol.Chem_286_28723 |
| PubMedID: 21665953 |
| Gene_locus related to this paper: human-ABHD6 |
| Gene_locus related to this paper: human-ABHD6 |
Marrs WR, Horne EA, Ortega-Gutierrez S, Cisneros JA, Xu C, Lin YH, Muccioli GG, Lopez-Rodriguez ML, Stella N (2011)
Dual inhibition of alpha\/beta-hydrolase domain 6 and fatty acid amide hydrolase increases endocannabinoid levels in neurons
Journal of Biological Chemistry
286 :28723
Marrs WR, Horne EA, Ortega-Gutierrez S, Cisneros JA, Xu C, Lin YH, Muccioli GG, Lopez-Rodriguez ML, Stella N (2011)
Journal of Biological Chemistry
286 :28723