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

Muneer Ahamed, Bala Attili, Daisy van Veghel, Maarten Ooms, Philippe Berben, Sophie Celen, Michel Koole, Lieven Declercq, Juha Savinainen, Jarmo Laitinen, Alfons Verbruggen, Guy Bormans

    Research output: Contribution to journalArticlepeer-review

    12 Citations (Scopus)

    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 languageEnglish
    Pages (from-to)104-113
    Number of pages10
    JournalEuropean Journal of Medicinal Chemistry
    Volume136
    Issue number18 August 2017
    DOIs
    Publication statusE-pub ahead of print - 2017

    Fingerprint Dive into the research topics of 'Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)'. Together they form a unique fingerprint.

    Cite this