LY2183240 is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis. It has been shown to increase anandamide levels in rat cerebellum (ED50 = 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 IC50 values of 33 and 998 nM, respectively.
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