Palmitoyl Ethanolamide

An AEA derivative; selectively activates PPARα (EC50 = 3.1 µM) over PPARβ/δ and PPARγ in HeLa cells expressing the human receptors; binds to RBL-2H3 basophil membranes (IC50 = 1 nM), which endogenously express CB2, but not CB1, receptors; inhibits antigen-induced serotonin release from RBL-2H3 cells (EC50 = 0.27 µM); prevents decreases in paw withdrawal latency in a radiant heat hypersensitivity test, an effect that can be reversed by SR141716, GW 9662, and capsazepine, in a mouse model of neuropathic pain induced by chronic constriction injury of the sciatic nerve; decreases carrageenan-induced paw edema in wild-type, but not Ppara-/-, mice at 10 mg/kg; inhibits PTZ-induced tonic convulsions in rats at 40 mg/kg