FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC 50 s of 11 nM and 36 nM ( K i s of 28 nM and 60 nM), respectively. FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment.