Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; Item No. 62160) and arachidonoyl ethanolamide (AEA; Item No. 90050) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid (CB) receptors. Fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) mediate the hydrolysis of AEA and 2-AG, respectively. MAGL inhibitor 21 selectively binds to MAGL (Ki = 0.4 µM) and reversibly blocks the enzyme’s activity in mouse brain with an IC50 value of 0.18 µM.{27369} Comparatively, MAGL inhibitor 21 is reported to inhibit FAAH activity in mouse brain with an IC50 value of 59 µM.{37369} This compound does not bind CB1 or CB2 receptors and does not inhibit the related serine hydrolases ABHD6 and ABHD12 (Kis > 10 µM).{27369} In a mouse model of multiple sclerosis, 5 mg/kg of MAGL inhibitor 21 has been used to ameliorate progression of the disease without producing detrimental CB1-mediated effects.{27369}
产品描述
Selectively and reversibly blocks MAGL activity (IC50s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis
