LY2183240
Anandamide uptake inhibitor / LY2183240 is highly potent inhibitor of cellular anandamide uptake (IC50 = 0.27nM1, 15nM2). LY2183240 has also been found2,3,4 to be an inhibitor of fatty acid amide hydrolase (FAAH) – IC50 = 14nM4, diacylglycerol lipase (DAGL) and monoacylglycerol lipase (MAGL) – IC50 = 5.3 nM3.
Biochemicals & reagents
874902-19-9
1) Moore et al., (2005), Identification of a high-affinity binding site involved in the transport of endocannabinoids; Proc.Natl.Acad.Sci.USA 102 17852 2) Ortar et al. (2008), Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revision; Eur.J.Med.Chem. 43 62 3) Alexander and Cravatt (2006), The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases; J.Am.Chem.Soc. 128 9699 4) Dickason-Chesterfield et al. (2006), Pharmacological Characterization of Endocannabinoid Transport and Fatty Acid Amide Hydrolase Inhibitors; Cell.Mol.Neurobiol. 26 405
-20°C
TARGET: Serine hydrolase -- PATHWAY: Cannabinoid receptor; Fatty acid metabolism -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Pain