Development of a novel ¹⁸F-labeled reversible-binding radioligand for imaging monoacylglycerol lipase with positron emission tomography.

ABSTRACT: Monoacylglycerol lipase (MAGL) constitutes a crucial serine hydrolase within the endocannabinoid system, which has been suggested as a potential therapeutic target for the treatment of various neurodegenerative disorders. While MAGL inhibitors have entered the clinical arena, a highly selective and MAGL-specific positron emission tomography (PET) ligand holds promise to significantly facilitate clinical drug development by allowing the quantification of MAGL levels and the assessment of target occupancy in patients. Accordingly, this study aimed to develop a new series of reversible MAGL inhibitor candidates, based on a piperazinyl azetidine diamide scaffold. Compound 3 demonstrated the most promising performance characteristics in pharmacological evaluations compared to other MAGL

SUBMITTER: Rong J 

PROVIDER: S-EPMC12750168 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature