Journal article Open Access

Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain Monoacylglycerol Lipase (MAGL)

Ahamed, Muneer; Atilli, Bala; van Veghel, Daisy; Ooms, Maarten; Berben, Philippe; Celen, Sofie; Koole, Michel; Declerq, Lieven; Savinainen, Juha R; Laitinen, Jarmo T; Verbruggen, Alfons; Bormans, Guy

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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