Abstract
MAGL is a potential therapeutic target for oncological and psychiatric diseases. Our objective was to develop a PET tracer for in vivo quantification of MAGL. We report [11C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, ex vivo distribution, brain kinetics and specificity of [11C]MA-PB-1 binding were studied. Ex vivo biodistribution and microPET showed good brain uptake which could be blocked by pretreatment with both MA-PB-1 and a structurally non-related MAGL inhibitor MJN110. These initial results suggest that [11C]MA-PB-1 is a suitable tracer for in vivo imaging of MAGL.
Original language | English |
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Pages (from-to) | 104-113 |
Number of pages | 10 |
Journal | European Journal of Medicinal Chemistry |
Volume | 136 |
Issue number | 18 August 2017 |
Early online date | 2017 |
DOIs | |
Publication status | Published - 2017 |
Keywords
- Biodistribution
- MAGL
- MJN110
- PET imaging
- [ C]MA-PB-1