The recent publication titles “Structure–Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors”. Monoacylglycerol lipase (MAGL) is the critical enzyme responsible for the hydrolysis of endocannabinoid 2-arachidonoylglycerol (2-AG) to arachidonate and glycerol, contributing to the inflammatory cascade in the CNS. MAGL inhibition provides various potential therapeutic opportunities, including inflammation-induced tissue injury, pain, multiple sclerosis, and cancer.
LEI-515 is an aryl sulfoxide, and a peripherally restricted, covalent reversible MAGL inhibitor. LEI-515 increases 2-AG levels in the periphery and reduces neuropathic pain and inflammation, without inducing CNS adverse effects or physical dependence.
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