OMDM-2 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a K_i of 3.0 μM^[1].

OMDM-2 shows poor affinity for either CB1 (K_i=5.1 μM) or CB2 (K_i>10 μM) receptors in rat brain and spleen membranes, respectively; OMDM-2 has almost no activity at vanilloid receptors in the intracellular calcium assay carried out with intact cells over-expressing the human VR1 (EC₅₀=10 μM), and no activity as inhibitors of FAAH in N18TG2 cell membranes (K_i>50 μM)^[1].