Published April 25, 2017
| Version v1
Journal article
Open
Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain Monoacylglycerol Lipase (MAGL)
Authors/Creators
- 1. Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
- 2. Department of Nuclear Medicine & Molecular Imaging, UZ Herestraat 49, 3000 Leuven, Belgium.
- 3. Institute of Biomedicine, Faculty of Health Sciences, The University of Eastern Finland, Finland.
Description
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.
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