OMDM169 is a potent and selective MAGL inhibitor. OMDM169 is capable of enhancing 2-AG levels and of exerting analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM10 microM) at human CB(1) and CB(2) receptors. OMDM69 might represent a template for the development of selective and even more potent inhibitors of 2-AG hydrolysis.