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

Biodistribution and stability studies of [18F]fluoroethylrhodamine B, a potential PET myocardial perfusion agent.
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DOI:
10.1016/j.nucmedbio.2009.12.005
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发表时间:
2010-04
影响因子:
3.1
通讯作者:
Packard AB
Packard AB
中科院分区:
医学4区
文献类型:
--
作者:
Gottumukkala V;Heinrich TK;Baker A;Dunning P;Fahey FH;Treves ST;Packard AB

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Fluorine-18-labeled rhodamine B was developed as a potential 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. [18F]Fluoroethylrhodamine B was equilibrated for 2 h at 37 °C in human, rat and mouse serum and in PBS. Samples were removed periodically and assayed by HPLC. Based on the results of the stability study, microPET imaging and a biodistribution study were carried out in rats. In vitro stability studies demonstrated that [18F]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 18F-labeled rhodamines should accumulate in the heart. [18F]Fluoroethyl rhodamine 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 18F-labeled rhodamines are promising candidates for more extensive evaluation as PET tracers for the evaluation of myocardial perfusion.
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