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MAGL-2102 is a novel, reversible monoacylglycerol lipase (MAGL) inhibitor developed as a positron emission tomography (PET) radiotracer (typically labeled as [18F]MAGL-2102) for in vivo neuroimaging of MAGL. MAGL is a key enzyme in the endocannabinoid system that degrades 2-arachidonoylglycerol (2-AG) into arachidonic acid, a precursor for proinflammatory eicosanoids. While preclinical studies in rodents and non-human primates showed promising brain uptake and specific binding, a first-in-human PET study demonstrated low brain penetration and high plasma protein binding in humans, suggesting that MAGL-2102 may have limited utility for reliable brain imaging of MAGL in clinical settings.
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