Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. Oleoyl oxazolopyridine is a potent inhibitor of FAAH exhibiting Ki values of 1.3 and 2.3 nM for the human and rat enzymes, respectively. Oleoyl oxazolopyridine is approximately 35-fold more potent than oleyl trifluoromethyl ketone when assayed under the same conditions. Selectivity of oleoyl oxazolopyridine for FAAH versus cannabinoid receptors or PLA2 has not been reported.