内源性大麻素过载。
Endocannabinoid overload.
机构信息
The Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA 23298, USA.
出版信息
Mol Pharmacol. 2010 Dec;78(6):993-5. doi: 10.1124/mol.110.069427. Epub 2010 Oct 15.
Abstract
The signaling capacity of endogenous cannabinoids ("endocannabinoids") is tightly regulated by degradative enzymes. This Perspective highlights a research article in this issue (p. 996) in which the authors show that genetic disruption of monoacylglycerol lipase (MAGL), the principal degradative enzyme for the endocannabinoid 2-arachidonoylglycerol (2-AG), causes marked elevations in 2-AG levels that lead to desensitization of brain cannabinoid receptors. These findings highlight the central role that MAGL plays in endocannabinoid metabolism in vivo and reveal that excessive 2-AG signaling can lead to functional antagonism of the brain cannabinoid system.
摘要
内源性大麻素（“内源性大麻素”）的信号转导能力受到降解酶的严格调节。本观点突出了本期杂志上的一篇研究文章（第 996 页），作者表明，单酰基甘油脂肪酶（MAGL）的基因缺失，MAGL 是内源性大麻素 2-花生四烯酸甘油（2-AG）的主要降解酶，会导致 2-AG 水平显著升高，从而导致大脑大麻素受体脱敏。这些发现强调了 MAGL 在体内内源性大麻素代谢中的核心作用，并揭示了过量的 2-AG 信号可能导致大脑大麻素系统的功能拮抗。
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