Solubility
JNJ 1661010 is soluble to 100 mM in DMSO and to 10 mM in ethanol.
Description
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.
Uses
JNJ-1661010, is used to examine the contribution of endocannabinoid signaling in experimental fibrosis. In biological studies, this compound had shown to elevate the levels of arachidonoyl ethanolamide (AEA) in rat brains.
Definition
ChEBI: JNJ-1661010 is a N-arylpiperazine.
Biological Activity
Selective, reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC 50 = 12nM). Brain penetrant and active in vivo .
References
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
