JNJ-1661010 (681136-29-8) is a potent and selective FAAH inhibitor. Initially forms a covalent adduct with FAAH but is slowly released, IC50 = 12 nM. 100-fold selectivity for FAAH-1 over FAAH-2. Cell permeable and active in vivo. JNJ-1661010 displays analgesic activity in various animal models.
1) Karbarz et al. (2009), Biochemical and biological properties of 4-(3-phenyl-[1,2,4]thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase; Anesth. Analg., 108 316