Monoacylglycerol Lipase Inhibitor 21 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; ) and arachidonoyl ethanolamide (AEA; ) 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. Monoacylglycerol Lipase 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. Comparatively, Monoacylglycerol Lipase Inhibitor 21 is reported to inhibit FAAH activity in mouse brain with an IC50 value of 59 μM. This compound does not bind CB1 or CB2 receptors and does not inhibit the related serine hydrolases ABHD6 and ABHD12 (Kis > 10 μM). In a mouse model of multiple sclerosis, 5 mg/kg of Monoacylglycerol Lipase Inhibitor 21 has been used to ameliorate progression of the disease without producing detrimental CB1-mediated effects.[Cayman Chemical]
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