Description
LY2183240 is a potent, competitive small molecule inhibitor of anandamide uptake (IC
50 = 270 pM; K
i = 540 pM) and hydrolysis. It has been shown to increase anandamide levels in rat cerebellum (ED
50 = 1.37 mg/kg) and displays dose-
dependent efficacy (3-
30 mg/kg) in several rodent models of persistent pain. LY2183240 2’-
isomer is a less potent, 2,5-
regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC
50 values of 33 and 998 nM, respectively.
Uses
5-([1,1''-Biphenyl]-4-ylmethyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide is an inhibitor of human monoacylglycerol lipase (hMGL).