2-Arachidonoyl glycerol (2-AG) is an endogenous agonist of the CB1 receptor. Unlike anandamide, 2-AG is present at relatively high levels in the central nervous system; it is the most abundant molecular species of monoacylglycerol found in rat brain. Formation of 2-AG is calcium-dependent and is mediated by the activities of PLC and DAG lipase. 2-AG acts as a full agonist at the CB1 receptor. At a concentration of 0.3 nM, 2-AG induces a rapid, transient increase in intracellular free calcium in NG108-15 neuroblastoma X glioma cells through a CB1 receptor-dependent mechanism. 2-AG is metabolized in vitro by MAG lipase and fatty acid amide hydrolase, with MAG lipase likely being the principle metabolizing enzyme in vivo.
产品描述
An analog of arachidonic acid in which the carboxyl group is replaced by a trifluoromethyl ketone group; inhibits the activity of the 85 kDa cPLA2 and the 80 kDa macrophage iPLA2 without altering the activity of the 14 kDa sPLA2s; at a concentration of 7.5 uM, almost completely inhibits hydrolysis of AEA in a rat brain homogenate