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Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels

Nomura, Daniel K., Hudak, Carolyn S.S., Ward, Anna M., Burston, James J., Issa, Roger S., Fisher, Karl J., Abood, Mary E., Wiley, Jenny L., Lichtman, Aron H. and Casida, John E. 2008. Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels. Bioorganic and Medicinal Chemistry Letters 18 (22) , pp. 5875-5878. 10.1016/j.bmcl.2008.08.007

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The structure–activity relationships of organophosphorus (OP) and organosulfur compounds were examined in vitro and in vivo as inhibitors of mouse brain monoacylglycerol lipase (MAGL) hydrolysis of 2-arachidonoylglycerol (2-AG) and agonist binding at the CB1 receptor. Several compounds showed exceptional potency toward MAGL activity with IC50 values of 0.1–10 nM in vitro and high inhibition at 10 mg/kg intraperitoneally in mice. We find for the first time that MAGL activity is a major in vivo determinant of 2-AG and arachidonic acid levels not only in brain but also in spleen, lung, and liver. Apparent direct OP inhibition of CB1 agonist binding may be due instead to metabolic stabilization of 2-AG in brain membranes as the actual inhibitor.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Medicine
Publisher: Elsevier
ISSN: 0960-894X
Date of Acceptance: 6 August 2008
Last Modified: 10 Jul 2018 14:31

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