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FAAH inhibitors act on fatty acid amide hydrolase (FAAH), a serine hydrolase that ends anandamide signaling. The enzyme was cloned in 1996 as a membrane protein that hydrolyzes oleamide, anandamide and related fatty acid amides. Inhibiting FAAH raises endogenous anandamide levels without directly binding cannabinoid receptors. In 2003, URB597 increased brain anandamide and produced anxiolytic-like effects in rats. PF-3845 and PF-04457845 are covalent FAAH inhibitors, and JNJ-42165279 and BIA 10-2474 extend the set. JZL195 inhibits both FAAH and monoacylglycerol lipase (MAGL) and also appears under Lipase. FP-Biotin is a biotinylated fluorophosphonate probe for activity-based profiling of serine hydrolases.
