NF 1819

NF 1819 is an irreversible inhibitor of monoacylglycerol lipase (MAGL, IC50s = 0. and 7. nM for the rat and human enzymes, respectively). It is selective for MAGL over fatty acid amide hydrolase (FAAH, IC50 = 2,880 nM for the human enzyme) and cannabinoid 1 (CB1) and CB2 receptors (IC50s = >10,000 nM for both). In vivo, NF 1819 (3 mg/kg) decreases disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE) induced by myelin oligodendrocyte glycoprotein (MOG) (35-55) (Cay-35644), an effect that can be reversed by AM251 (Cay-71670) or AM630 (Cay-10006974). It induces analgesia in the formalin test in mice when administered at a dose of 0. mg/kg. NF 1819 (3 mg/kg) inhibits LPS-induced motor and cognitive impairments in the rotarod and passive avoidance tests, respectively, and LPS-induced depressive-like behavior in the forced swim test, in mice. It increases the number of entries into and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, in a rat model of predator stress-induced anxiety using the fox pheromone 2,5-dihydro-2,4,5-trimethylthiazoline (TMT).. Solulibility: DMSO: Soluble:= 10 mg/ml: Ethanol: Soluble: = 10 mg/ml.