URB754 is an endogenous agonist of the central cannabinoid (CB1) receptor.It is present at relatively high levels in the central nervous system and is the most abundant molecular species of monoacylglycerol found in rat brain.Monoacylglycerol lipase (MGL) hydrolyzes 2-AG to arachidonic acid and glycerol, thereby terminating its biological actions.URB754 is reported to be a potent, noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 of 200 nM for the recombinant rat brain enzyme.However, data from other labs indicates that it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 µM.It inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 of 32 µM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 of 3.8 µM.It does not inhibit cyclooxygenase-1 (COX-1) or COX-2 at concentrations up to 100 µM.Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.