NF 1819

NF 1819 is an irreversible inhibitor of monoacylglycerol lipase (MAGL; IC₅₀s = 0.25 and 7.4 nM for the rat and human enzymes, respectively).¹ 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) (Item No. 35644), an effect that can be reversed by AM251 (Item No. 71670) or AM630 (Item No. 10006974). It induces analgesia in the formalin test in mice when administered at a dose of 0.3 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.² 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).³

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1. Brindisi, M., Maramai, S., Gemma, S., et al. Development and pharmacological characterization of selective blockers of 2-arachidonoyl glycerol degradation with efficacy in rodent models of multiple sclerosis and pain. J. Med. Chem. 59(6), 2612-2632 (2016).

2. Micheli, L., Maramai, S., Toti, A., et al. Inhibition of monoacylglycerol lipase by NSD1819 as an effective strategy for the endocannabinoid system modulation against neuroinflammation-related disorders. Int. J. Mol. Sci. 23(15), 8428 (2022).

3. Lim, J., Igarashi, M., Jung, K.-M., et al. Endocannabinoid modulation of predator stress-induced long-term anxiety in rats. Neuropsychopharmacology 41(5), 1329-1339 (2016).