The enzyme fatty acid amide hydrolase (FAAH) is widely expressed in brain and other tissues, and is capable of hydrolyzing anandamide (AEA) and other simple esters and amides with long unsaturated acyl chains.1 URB597 was recently synthesized and reported to be a potent and selective inhibitor of FAAH.2 URB597 inhibits FAAH with an IC50 of 4.6 nM in brain membranes and 0.5 nM in intact neurons. It has been demonstrated in FAAH(-/-) mice that marked depression of FAAH activity results in reduced sensation of pain and enhanced endocannabinoid signalling.3 URB597 exhibits both anti-nociceptive and anxiolytic effects in vivo without evoking other symptoms associated with cannabinoid-like compounds. Thus, URB597 may serve as a lead compound for the development of new analgesic and anxiolytic drugs.
1Cravatt, B.F., Giang, D.K., Mayfield, S.P., et al. Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides. Nature38483-87(1996).
2Kathuria, S., Gaetani, S., Fegley, D., et al. Modulation of anxiety through blockade of anandamide hydrolysis. Nat Med1(9)76-81(2003).
3Cravatt, 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 USA98(16)9371-9376(2001).
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Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.
Manufacturer, supplier, and vendor of biochemical reagents, assay kits, forensic chemistry standards, antibodies, and proteins for scientific research
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