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, Sofie Celen, Michel Koole, Lieven Declercq, Juha R. Savinainen, Jarmo T. Laitinen, Alfons Verbruggen, Guy Bormans

Research output: Contribution to journalArticlepeer-review

21 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
DOIs
Publication statusPublished or Issued - 2017
Externally publishedYes

Keywords

  • Biodistribution
  • MAGL
  • MJN110
  • PET imaging
  • [C]MA-PB-1

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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