URB754 was originally reported by Piomelli ''et al.'' to be a potent, noncompetitive
inhibitor of
monoacylglycerol lipase
Monoacylglycerol lipase (EC 3.1.1.23; systematic name glycerol-ester acylhydrolase, also known as MAG lipase, acylglycerol lipase, MAGL, MGL or MGLL) is an enzyme that, in humans, is encoded by the ''MGLL'' gene. MAGL is a 33-kDa, membrane-associ ...
(MGL).
However, recent studies have shown that URB754 failed to inhibit recombinant MGL, and brain
FAAH activity was also resistant to URB754. In a later study by Piomelli ''et al.'', the MGL-inhibitory activity attributed to URB754 is in fact due to a chemical impurity present in the commercial sample, identified as bis(methylthio)mercurane.
References
Benzoxazines
Lactones
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