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

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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… Click to show full 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: potential nonpeptidic; tracer imaging; ccr2 receptors; imaging ccr2; development; first potential

Journal Title: Chemmedchem
Year Published: 2020

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