Numerous analogs of arachidonoyl ethanolamide (AEA, anandamide; ) potentiate its biological activity. This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty acid amide hydrolase (FAAH) within the neurons. OMDM-2 is an endocannabinoid analog specifically designed to be a potent and selective inhibitor of the cellular uptake of AEA. Structurally, OMDM-2 is the amide of (R)-tyrosinol with oleic acid. In RBL-2H3 cells, OMDM-2 inhibits the cellular uptake of tritiated AEA with an IC50 of 3 μM, with negligible effects on the CB1 receptor and VR1.
