The serine hydrolase ABHD6 controls the accumulation and efficacy of 2-AG at cannabinoid receptors

被引:335
作者
Marrs, William R. [2 ]
Blankman, Jacqueline L. [3 ,4 ]
Horne, Eric A. [1 ]
Thomazeau, Aurore [5 ]
Lin, Yi Hsing [1 ]
Coy, Jonathan [1 ]
Bodor, Agnes L. [6 ]
Muccioli, Giulio G. [7 ]
Hu, Sherry Shu-Jung [8 ]
Woodruff, Grace [9 ]
Fung, Susan [2 ]
Lafourcade, Mathieu [5 ]
Alexander, Jessica P. [3 ,4 ]
Long, Jonathan Z. [3 ,4 ]
Li, Weiwei [3 ,4 ]
Xu, Cong [1 ]
Moeller, Thomas [10 ]
Mackie, Ken [8 ]
Manzoni, Olivier J. [5 ]
Cravatt, Benjamin F. [3 ,4 ]
Stella, Nephi [1 ,11 ]
机构
[1] Univ Washington, Dept Pharmacol, Seattle, WA 98195 USA
[2] Univ Washington, Neurobiol & Behav Grad Program, Seattle, WA 98195 USA
[3] Scripps Res Inst, Dept Physiol Chem, La Jolla, CA 92037 USA
[4] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
[5] Equipe Physiopathol Plast Synapt, INSERM, U862, Bordeaux, France
[6] Univ Washington, Dept Otolaryngol, Seattle, WA 98195 USA
[7] Catholic Univ Louvain, Louvain Drug Res Inst, CHAM7230, Bioanal & Pharmacol Bioact Lipids Lab, B-1200 Brussels, Belgium
[8] Indiana Univ, Gill Ctr Biomol Sci, Dept Psychol & Brain Sci, Bloomington, IN USA
[9] Univ Washington, Neurobiol Undergraduate Program, Seattle, WA 98195 USA
[10] Univ Washington, Dept Neurol, Seattle, WA 98195 USA
[11] Univ Washington, Dept Psychiat & Behav Sci, Seattle, WA 98195 USA
关键词
2-ARACHIDONOYLGLYCEROL HYDROLYSIS; ENDOGENOUS CANNABINOIDS; ENDOCANNABINOID SYSTEM; ANANDAMIDE; BLOCKADE; BRAIN; MODULATION; ACID; INHIBITOR; ENZYMES;
D O I
10.1038/nn.2601
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
The endocannabinoid 2-arachidonoylglycerol (2-AG) regulates neurotransmission and neuroinflammation by activating CB1 cannabinoid receptors on neurons and CB2 cannabinoid receptors on microglia. Enzymes that hydrolyze 2-AG, such as monoacylglycerol lipase, regulate the accumulation and efficacy of 2-AG at cannabinoid receptors. We found that the recently described serine hydrolase alpha-beta-hydrolase domain 6 (ABHD6) also controls the accumulation and efficacy of 2-AG at cannabinoid receptors. In cells from the BV-2 microglia cell line, ABHD6 knockdown reduced hydrolysis of 2-AG and increased the efficacy with which 2-AG can stimulate CB2-mediated cell migration. ABHD6 was expressed by neurons in primary culture and its inhibition led to activity-dependent accumulation of 2-AG. In adult mouse cortex, ABHD6 was located postsynaptically and its selective inhibition allowed the induction of CB1-dependent long-term depression by otherwise subthreshold stimulation. Our results indicate that ABHD6 is a rate-limiting step of 2-AG signaling and is therefore a bona fide member of the endocannabinoid signaling system.
引用
收藏
页码:951 / U67
页数:9
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