Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors. (23rd November 2020)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: ChemMedChem. Volume 16:Number 4(2021)
• Page Start: 640
• Page End: 645
• Publication Date: 2020-11-23
• Subjects: CCR2 -- CCR5 antagonists -- chemokine receptors -- molecular imaging -- PET -- radiolabeling -- TAK-779; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.202000728
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract: 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. Abstract : Off target, on track : Highly selective CCR2 antagonists have been designed and synthesized as 18 F‐labeled PET tracers and evaluated extensively for their off‐target profile targets. A promising profile for further preclinical development was demonstrated by the most potent and selective candidate in an in vivo biodistribution study. This compound is the first potential nonpeptidic PET tracer for imaging CCR2 receptors.