LY2183240 is a highly potent blocker of anandamide uptake with IC50 of 270 pM in cellular assay.
LY2183240 inhibits the putative endocannabinoid (EC) transporter, and disrupts the cellular uptake of the lipid EC anandamide and promote analgesia in vivo.
LY2183240 proved to be a potent, covalent inhibitor of EC-degrading enzyme FAAH (IC50=12.4 nM) and and several other serine hydrolases in vivo (MAGL, α/β-hydrolase 6, KIAA1363).
