Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases

…, X Jin, A Adibekian, W Li, BF Cravatt

Index: Long, Jonathan Z.; Jin, Xin; Adibekian, Alexander; Li, Weiwei; Cravatt, Benjamin F. Journal of Medicinal Chemistry, 2010 , vol. 53, # 4 p. 1830 - 1842

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Citation Number: 40

Abstract

Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) are two enzymes from the serine hydrolase superfamily that degrade the endocannabinoids 2- arachidonoylglycerol and anandamide, respectively. We have recently discovered that MAGL and FAAH are both inhibited by carbamates bearing an N-piperidine/piperazine group. Piperidine/piperazine carbamates show excellent in vivo activity, raising brain ...