URB597

URB597 is a potent and selective inhibitor of fatty acid amide hydrolase (FAAH), the enzyme that hydrolyzes anandamide (AEA; Item No. 90050) and other simple esters and amides with long unsaturated acyl chains (IC₅₀ = 4.6 nM and 0.5 nM in brain membranes and intact neurons, respectively).^1,2 URB597 exhibits both antinociceptive and anxiolytic effects in vivo without evoking other symptoms associated with cannabinoid-like compounds. This antinociceptive effect is similar to those observed in FAAH^(-/-) mice.³

WARNING This product is not for human or veterinary use.

1. Kathuria, S., Gaetani, S., Fegley, D., et al. Modulation of anxiety through blockade of anandamide hydrolysis. Nat. Med. 1(9), 76-81 (2003).

2. Cravatt, B.F., Giang, D.K., Mayfield, S.P., et al. Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides. Nature 384(6604), 83-87 (1996).

3. Cravatt, B.F., Demarest, K., Patricelli, M.P., et al. Supersensitivity to anandamide and enhanced endogenous cannabinoid signaling in mice lacking fatty acid amide hydrolase. Proc. Natl. Acad. Sci. USA 98(16), 9371-9376 (2001).

Soethoudt, M., Grether, U., Fingerle, J., et al. Cannabinoid CB₂ receptor ligand profiling reveals biased signalling and off-target activity. Nat. Commun. 8, 13958 (2017).

Gouveia-Figueira, S., Karlsson, J., Deplano, A., et al. Characterisation of (R)-2-(2-fluorobiphenyl-4-yl)-N-(3-methylpyridin-2-yl)propanamide as a dual fatty acid amide hydrolase: Cyclooxygenase inhibitor. PLoS One 10(9), e0139212 (2015).