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• W2913635060 endingPage "2375" @default.
• W2913635060 startingPage "2362" @default.
• W2913635060 abstract "Monoacylglycerol lipase (MAGL) is a cytosolic serine hydrolase involved in endocannabinoid and inflammatory signaling. Positron-emission tomography (PET) imaging of MAGL serves to validate target engagement of therapeutic MAGL inhibitors as well as to investigate MAGL levels under normal and disease conditions. However, PET radioligands with reversible binding kinetics for MAGL, which allow quantitative assessment of MAGL, are hitherto unavailable. In this study, we designed and synthesized fluoro-containing PET probes starting from a recently identified piperazinyl pyrrolidine-2-one derivative with reversible binding to MAGL. By tailoring the lipophilicity of the molecule to optimize nonspecific binding and blood–brain barrier permeability, we successfully identified two compounds that show high uptake to regions enriched with MAGL. PET imaging of wild-type and MAGL-deficient mice as well as a macaque monkey indicated that [18F]5 ((4R)-1-{3-[2-(18F)fluoro-4-methylpyridin-3-yl]phenyl}-4-[4-(1,3-thiazol-2-ylcarbonyl)piperazin-1-yl]pyrrolidin-2-one, [18F]T-401) specifically binds to MAGL with adequate reversibility, yielding a high contrast for MAGL within an appropriate imaging time." @default.
• W2913635060 created "2019-02-21" @default.
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• W2913635060 date "2019-02-12" @default.
• W2913635060 modified "2023-10-17" @default.
• W2913635060 title "Design, Synthesis, and Evaluation of (4<i>R</i>)-1-{3-[2-(¹⁸F)Fluoro-4-methylpyridin-3-yl]phenyl}-4-[4-(1,3-thiazol-2-ylcarbonyl)piperazin-1-yl]pyrrolidin-2-one ([¹⁸F]<b>T-401</b>) as a Novel Positron-Emission Tomography Imaging Agent for Monoacylglycerol Lipase" @default.
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• W2913635060 doi "https://doi.org/10.1021/acs.jmedchem.8b01576" @default.
• W2913635060 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30753069" @default.
• W2913635060 hasPublicationYear "2019" @default.
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