Development of the first potential nonpeptidic positron emission tomography tracer for the imaging of CCR2 receptors

Wagner, S.; Moura Gatti, F.; Silva, D.G. de; Ortiz Zacarias, N.V.; Zweemer, A.J.M.; Hermann, S.; Maria M. de; Koch, M.; Weiss, C.; Schepmann, D.; Heitman, L.H.; Tschammer, N.; Kopka, K.; Junker, A.

doi:doi:10.1002/cmdc.202000728

Persistent URL of this record https://hdl.handle.net/1887/3134856

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Leiden Academic Centre for Drug Research (LACDR)

Wagner, S.; Moura Gatti, F.; Silva, D.G. de; Ortiz Zacarias, N.V.; Zweemer, A.J.M.; Hermann, S.; ... ; Junker, A. (2020)

Development of the first potential nonpeptidic positron emission tomography tracer for the imaging of CCR2 receptors

Article / Letter to editor

Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as¹⁸F‐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.