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Comparative Study
. 2010 Apr;37(3):365-70.
doi: 10.1016/j.nucmedbio.2009.12.005. Epub 2010 Feb 10.

Biodistribution and stability studies of [18F]fluoroethylrhodamine B, a potential PET myocardial perfusion agent

Vijay Gottumukkala  1 , Tobias K Heinrich, Amanda Baker, Patricia Dunning, Frederic H Fahey, S Ted Treves, Alan B Packard
Affiliations
Comparative Study

Biodistribution and stability studies of [18F]fluoroethylrhodamine B, a potential PET myocardial perfusion agent

Vijay Gottumukkala et al. Nucl Med Biol. 2010 Apr.

Abstract

Introduction: Fluorine-18-labeled rhodamine B was developed as a potential positron emission tomography (PET) tracer for the evaluation of myocardial perfusion, but preliminary studies in mice showed no accumulation in the heart suggesting that it was rapidly hydrolyzed in vivo in mice. A study was therefore undertaken to further evaluate this hypothesis.

Methods: [(18)F]Fluoroethylrhodamine B was equilibrated for 2 h at 37 degrees C in human, rat and mouse serum and in phosphate-buffered saline. Samples were removed periodically and assayed by high-performance liquid chromatography. Based on the results of the stability study, microPET imaging and a biodistribution study were carried out in rats.

Results: In vitro stability studies demonstrated that [(18)F]fluoroethylrhodamine B much more stable in rat and human sera than in mouse serum. After 2 h, the compound was >80% intact in rat serum but <30% intact in mouse serum. The microPET imaging and biodistribution studies in rats confirmed this result showing high and persistent tracer accumulation in the myocardium compared with the absence of uptake by the myocardium in mice thereby validating our original hypothesis that (18)F-labeled rhodamines should accumulate in the heart.

Conclusions: [(18)F]Fluoroethylrhodamine B is more stable in rat and human sera than it is in mouse serum. This improved stability is demonstrated by the high uptake of the tracer in the rat heart in comparison to the absence of visible uptake in the mouse heart. These observations suggest that (18)F-labeled rhodamines are promising candidates for more extensive evaluation as PET tracers for the evaluation of myocardial perfusion.

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Figures

Figure 1
Figure 1
2′-Fluoroethylrhodamine B
Figure 2
Figure 2
Stability of 2′-[18F]fluoroethylrhodamine B in various sera
Figure 3
Figure 3
Sample HPLC chromatograms of serum samples. Chromatograms were smoothed using the Savistsky-Golay method (20 neighbors, 2nd order)
Figure 4
Figure 4
MicroPET images of a rat injected with 2′-[18F]fluoroethylrhodamine B.
Figure 5
Figure 5
Time activity curve of a rat myocardium and liver after injection with 2′-[18F]fluoroethylrhodamine B
See this image and copyright information in PMC

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