Document Report Card

ID: ALA2163210

Journal: ACS Med Chem Lett

Title: Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate.

Authors: Keith JM, Apodaca R, Tichenor M, Xiao W, Jones W, Pierce J, Seierstad M, Palmer J, Webb M, Karbarz M, Scott B, Wilson S, Luo L, Wennerholm M, Chang L, Brown S, Rizzolio M, Rynberg R, Chaplan S, Breitenbucher JG.

Abstract: A series of aryl piperazinyl ureas that act as covalent inhibitors of fatty acid amide hydrolase (FAAH) is described. A potent and selective (does not inhibit FAAH-2) member of this class, JNJ-40355003, was found to elevate the plasma levels of three fatty acid amides: anandamide, oleoyl ethanolamide, and palmitoyl ethanolamide, in the rat, dog, and cynomolgous monkey. The elevation of the levels of these lipids in the plasma of monkeys suggests that FAAH-2 may not play a significant role in regulating plasma levels of fatty acid ethanolamides in primates.

CiteXplore: 24900385

DOI: 10.1021/ml300186g