Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors


Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors

Wagner, S.; De, M. G. F.; Silva, D.; Ortiz, Z. N.; Zweemer, A.; Hermann, S.; De, M. M.; Koch, M.; Weiss, C.; Schepmann, D.; Heitman, L.; Tschammer, N.; Kopka, K.; Junker, A.

Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as 18F-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.

Keywords: CCR2; CCR5 antagonists; chemokine receptors; molecular imaging; PET; radiolabeling; TAK-779

Permalink: https://www.hzdr.de/publications/Publ-31767
Publ.-Id: 31767