URB754 is a potent, noncompetitive inhibitor of MGL, exhibiting an IC50 of 200 nM for the recombinant rat brain enzyme. It inhibits rat brain fatty acyl amide hydrolase (FAAH) less effectively with an IC50 of 32 µM and binds weakly to the rat CB1 receptor with an IC50 of 3.8 µM. It does not inhibit cyclooxygenase-1 (COX-1) or COX-2 at concentrations up to 100 µM. Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.
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