OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM<IC(50)<0.41 microM towards 2-AG hydrolysing activities in rat cerebellum and COS-7 cells, and inhibited the human recombinant MAGL (IC(50)=0.89 microM), whilst being inactive at human CB(1) and CB(2) receptors (K(i)>10 microM).