Inhibitors and Assay
The enzyme was reported to be inhibited by URB754; however this inhibitor has subsequently been shown to be inactive and its reported activity due to contamination. While the compound N-arachidonoyl maleimide (NAM) inhibits MAGL, NAM is not selective due to its chemically reactive maleimide functional group, which can also react with other thiol-containing small molecules and proteins (e.g., glutathione).
JZL184 is the first efficacious and selective inhibitor of MAGL that can elevate brain 2-AG levels in vivo. JZL184 has >300-fold selectivity for MAGL over other brain serine hydrolases, including FAAH.
MAGL activity is commonly detected by measuring free fatty acid release from a monoacylglycerol substrate using a liquid chromatography mass spectrometry system or the radiolabelled substrate 2-oleoyl--glycerol.
Read more about this topic: Monoacylglycerol Lipase
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