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

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 s...

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Detalles Bibliográficos
Autores principales: Wagner, Stefan, de Moura Gatti, Fernando, Silva, Daniel G., Ortiz Zacarias, Natalia V., Zweemer, Annelien J. M., Hermann, Sven, De Maria, Monica, Koch, Michael, Weiss, Christina, Schepmann, Dirk, Heitman, Laura H., Tschammer, Nuska, Kopka, Klaus, Junker, Anna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Full Papers
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7983900/
https://www.ncbi.nlm.nih.gov/pubmed/33205603
http://dx.doi.org/10.1002/cmdc.202000728
Descripción
Sumario: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.

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