Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors.
Stefan WagnerFernando de Moura GattiDaniel Gedder SilvaNatalia V Ortiz ZacariasAnnelien J M ZweemerSven HermannMonica De MariaMichael KochChristina WeissDirk SchepmannLaura H HeitmanNuska TschammerKlaus KopkaAnna JunkerPublished in: ChemMedChem (2020)
Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as 18 F-labeled PET tracers. The derivatives were evaluated extensively for their off-target profile at 48 different targets. The most potent and selective candidate was applied in vivo in a biodistribution study, demonstrating a promising profile for further preclinical development. This compound represents the first potential nonpeptidic PET tracer for the imaging of CCR2 receptors.