Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-
arachidonoyl glycerol (2-
AG), terminating its capacity to activate cannabinoid receptors. Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC
50 = 93 nM).
1 Its actions are rapid, reversible, and noncompetitive.
1 Pristimerin (1 μM) significantly increases 2-
AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells.
1 Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).