1010096-65-7

LY2183240 is a potent, competitive small molecule inhibitor of anandamide uptake (IC₅₀ = 270 pM; K_i = 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.

5-([1,1''-Biphenyl]-4-ylmethyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide is an inhibitor of human monoacylglycerol lipase (hMGL).

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[1] S A MOORE. Identification of a high-affinity binding site involved in the transport of endocannabinoids.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 49: 17852-17857. DOI: 10.1073/pnas.0507470102
[2] GIORGIO ORTAR . Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revisitation[J]. European Journal of Medicinal Chemistry, 2008, 43 1: Pages 62-72. DOI: 10.1016/j.ejmech.2007.02.023
[3] MARZO V D. Targeting the endocannabinoid system: to enhance or reduce?[J]. Nature Reviews. Drug Discovery, 2008, 7 5: 438-455. DOI: 10.1038/nrd2553