Linoleoyl glycine is an endogenous homolog of linoleoyl ethanolamide, an arachidonyl glycine. Arachidonyl glycine, the conjugate of arachidonic acid and glycine produced in mammalian skin, spinal cord and brain, is a structural counterpart of anandamide (AEA) that is reported to have analgesic activities in whole animal experiments. It has poor affinity for the central cannabinoid (CB1) receptor, high-affinity for the G protein-coupled receptor GPR-18, and is metabolically regulated by fatty acid amide hydrolase (FAAH) activity. Linoleoyl glycine inhibits the hydrolysis of AEA in FAAH-containing N18TG2 cell membranes (IC50 ~ 25 M), which is less potent than that of arachidonyl glycine (IC50 = 7 M). The biological significance of linoleoyl glycine has not yet been determined.
