CNS-active, potent and selective inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD)
LEI-401 is a CNS-active, potent and selective inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD). LEI-401 reduces N-acylethanolamines (NAEs) in in the brain of freely moving mice and neuroblastoma cells.
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Journal of medicinal chemistry, 64(1), 481-515 (2021-01-01)
N-Acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is regarded as the main enzyme responsible for the biosynthesis of N-acylethanolamines (NAEs), a family of bioactive lipid mediators. Previously, we reported N-(cyclopropylmethyl)-6-((S)-3-hydroxypyrrolidin-1-yl)-2-((S)-3-phenylpiperidin-1-yl)pyrimidine-4-carboxamide (1, LEI-401) as the first potent and selective NAPE-PLD inhibitor that decreased NAEs
Nature chemical biology, 16(6), 667-675 (2020-05-13)
N-acylethanolamines (NAEs), which include the endocannabinoid anandamide, represent an important family of signaling lipids in the brain. The lack of chemical probes that modulate NAE biosynthesis in living systems hamper the understanding of the biological role of these lipids. Using
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