2016年3月
Radiosynthesis and preliminary biological evaluation of a new F-18-labeled triethylene glycol derivative of triphenylphosphonium
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
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- 巻
- 59
- 号
- 3
- 開始ページ
- 117
- 終了ページ
- 123
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1002/jlcr.3379
- 出版者・発行元
- WILEY-BLACKWELL
Delocalized lipophilic cations such as [F-18]fluorobenzyltriphenylphosphonium ([F-18]FBnTP) can accumulate in mitochondria and have been used in myocardial perfusion imaging (MPI). In this study, we established a simplified method for [F-18]FBnTP synthesis using triphenylphosphine hydrobromide (PPh3 center dot HBr) without preparing an intermediate that contains benzyl bromide structure. Applying this new method, we synthesized and evaluated a novel F-18-labeled PEGylated BnTP derivative ([F-18]FPEGBnTP). In vitro cellular uptake study demonstrated that [F-18]FPEGBnTP accumulated in cells in proportion to the relative intensity of mitochondrial membrane potential. Biodistribution study revealed that the heart:liver uptake ratio of [F-18]FPEGBnTP (4.00 at 60min) was superior to that of [F-18]FBnTP (1.50 at 60min). However, [F-18]FPEGBnTP showed slow blood clearance and high radioactivity uptake in bone at 120-min post-injection. These results imply the possibility of [F-18]FPEGBnTP being used as a MPI agent. However, there is a need of further structural optimization and flow-dependent uptake study.
- リンク情報
- ID情報
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- DOI : 10.1002/jlcr.3379
- ISSN : 0362-4803
- eISSN : 1099-1344
- Web of Science ID : WOS:000372328200006