An NAPE-PLD inhibitor
LEI-401 is an inhibitor of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD; IC50 = 0.86 ?M in HEK293T cell membranes expressing the recombinant human enzyme).1 It is selective for NAPE-PLD over human cannabinoid (CB) receptor 1 (CB1), CB2, type IVE phospholipase A2, monoacylglycerol lipase (MAGL), and diacylglycerol lipase α (DAGLα), as well as mouse DAGLα, DAGLβ, fatty acid amide hydrolase (FAAH), and α/β-hydrolase domain-containing protein 6 (ABHD6), at 10 ?M. LEI-401 (10 ?M) reduces levels of a variety of N-acylethanolamines (NAEs), including N-palmitoylethanolamine (PEA), N-oleoylethanolamine (OEA), and N-arachidonoylethanolamine , in Neuro2a cells. It impairs fear extinction in a cued fear conditioning test in mice when administered at a dose of 30 mg/kg.
1.Mock, E.D., Mustafa, M., Gunduz-Cinar, O., et al.Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in miceNat. Chem. Biol.16(6)667-675(2020)
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