Methanone, [4-(2'-Methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylMethyl)-1-piperidinyl]-

BeschreibungKT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ. It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC50s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC50 = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 μM. KT172 decreases production of 2-arachidonoyl glycerol and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E2 (PGE2; ), and PGD2 in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.