10.1002/cmdc.202000085
ChemMedChem
COMMUNICATION
Experimental section
Experimental procedures for the chemistry and in vitro
autoradiography are presented as supplementary information.
Acknowledgments
We thank Dr. Susan Bengs for providing the rodent tissue.
Keywords: Flurpiridaz • Imaging agents • Myocardial perfusion
imaging • Positron emission tomography • Synthetic methods
Figure 1. Representative in vitro autoradiography of mouse heart tissue
sections incubated with [18F]flurpiridaz under baseline and blockade conditions.
Blocking was achieved with either MC-1 ligand, rotenone, or flurpiridaz.
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Figure 2. Quantification of specific binding of [18F]flurpiridaz calculated from the
in vitro autoradiographic assessment.
In summary, we have successfully synthesized precursor 13 in
five steps with an overall yield of 37%, which is more than five-
fold higher compared to the previously reported procedure
comprising of six steps. Furthermore, the use of hazardous and
toxic ethylene oxide was avoided and supplemented using readily
available reagents. Our improved synthetic route is more suitable
for large-scale synthesis. Using in vitro autoradiography, we also
demonstrated the high specific binding of [18F]flurpiridaz towards
MC-1 in the mouse myocardium, thus paving the way for the
assessment of MBF and CFR in various existing mouse models
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