Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)
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CitationAhamed Muneer. Attili Bala. van Veghel Daisy. Ooms Maarten. Berben Philippe. Celen Sofie. Koole Michel. Declercq Lieven. Savinainen Juha R. Laitinen Jarmo T. Verbruggen Alfons. Bormans Guy. (2017). Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL). EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 136, 104-113. 10.1016/j.ejmech.2017.04.066.
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.
SubjectsMAGL [11C]MA-PB-1 MJN110 Biodistribution PET imaging
Link to the original itemhttp://dx.doi.org/10.1016/j.ejmech.2017.04.066
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