論文

査読有り
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
  • Takahiro Tominaga
  • ,
  • Hiroaki Ito
  • ,
  • Yoichi Ishikawa
  • ,
  • Ren Iwata
  • ,
  • Kiichi Ishiwata
  • ,
  • Shozo Furumoto

59
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
DOI
https://doi.org/10.1002/jlcr.3379
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000372328200006&DestApp=WOS_CPL
ID情報
  • DOI : 10.1002/jlcr.3379
  • ISSN : 0362-4803
  • eISSN : 1099-1344
  • Web of Science ID : WOS:000372328200006

エクスポート
BibTeX RIS