2-Arachidonoyl Glycerol

2-Arachidonoyl glycerol (2-AG) is an endogenous agonist of the cannabinoid (CB) receptors CB1 and CB2 (Kis = 25.3-472 and 145-1,400 nM, respectively).{7183,7182,7912} Unlike arachidonoyl ethanolamide (AEA; Item No. 90050), 2-AG is present at relatively high levels in the central nervous system and is the most abundant molecular species of monoacylglycerol (MAG) found in rat brain.{7183,6819} Formation of 2-AG is calcium-dependent and is mediated by the activities of phospholipase C (PLC) and diacylglycerol (DAG) lipase.{7183} 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.{7182} 2-AG is metabolized in vitro by MAG lipase and fatty acid amide hydrolase (FAAH), with MAG lipase likely being the principle metabolizing enzyme in vivo.{11364}