Publikationsrepositorium - Helmholtz-Zentrum Dresden-Rossendorf

1 Publikation

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.

Abstract

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