Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 22, Issue 34, Pages 12122-12129Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201601972
Keywords
BODIPY; dual-modality imaging; fluorine-18; medicinal chemistry; radiopharmaceuticals
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Funding
- National Cancer Institute [P30-CA016086-35-37]
- Biomedical Research Imaging Center, University of North Carolina at Chapel Hill
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Recently, we demonstrated the potential of a [F-18]-trimethylammonium BODIPY dye for cardiac imaging. This is the first example of the use of the [F-18]-ammonium BODIPY dye for positron emission tomography (PET) myocardial perfusion imaging (MPI). In this report, we extend our study to other ammonium BODIPY dyes with different nitrogen substituents. These novel ammonium BODIPY dyes were successfully prepared and radiolabeled by the SnCl4-assisted F-18-F-19 isotopic exchange method. The microPET results and the biodistribution data reveal that nitrogen substituent changes have a significant effect on the in vivo and pharmacological properties of the tracers. Of the novel [F-18]-ammonium BODIPY dyes prepared in this work, the [F-18]-dimethyl-ethylammonium BODIPY is superior in terms of myocardium uptake and PET imaging contrast. These results support our hypothesis that the ammonium BODIPY dyes have a great potential for use as PET/optical dual-modality MPI probes.
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