論文

2019年7月

Fluorine-18 (F-18)-labeled retinoid x receptor (RXR) partial agonist whose tissue transferability is affected by other RXR ligands

BIOORGANIC & MEDICINAL CHEMISTRY
  • Yuta Takamura
  • ,
  • Osamu Shibahara
  • ,
  • Masaki Watanabe
  • ,
  • Michiko Fujihara
  • ,
  • Shoya Yamada
  • ,
  • Masaru Akehi
  • ,
  • Takanori Sasaki
  • ,
  • Hiroyuki Hirano
  • ,
  • Hiroki Kakuta

27
14
開始ページ
3128
終了ページ
3134
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bmc.2019.05.045
出版者・発行元
PERGAMON-ELSEVIER SCIENCE LTD

Bexarotene (1), a retinoid X receptor (RXR) agonist approved for the treatment of cutaneous T cell lymphoma (CTCL), was reported to migrate into baboon brain based on findings obtained by positron emission tomography (PET) with a C-11-labeled tracer. However, co-administration of non-radioactive 1 had no effect on the distribution of [C-11]1, probably due to non-specific binding of 1 as a result of its high lipophilicity. Here, we report a fluorine-18 (F-18)-labeled PET tracer [F-18] 6 derived from RXR partial agonist CBt-PMN (2), which has lower lipophilicity and weaker RXR-binding ability than [C-11]1. The concomitant administration of 1 or 2 with [F-18]6 with resulted in decreased accumulation of [F-18]6 in liver, together with increased brain uptake and increased accumulation in kidney and muscle, as visualized by PET. A plausible explanation of these findings is the inhibition of [F-18]6 uptake into the liver by concomitantly administered 1 or 2, leading to an increase in blood concentration of [F-18]6 followed by increased accumulation in other tissues.

リンク情報
DOI
https://doi.org/10.1016/j.bmc.2019.05.045
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000476649000009&DestApp=WOS_CPL
ID情報
  • DOI : 10.1016/j.bmc.2019.05.045
  • ISSN : 0968-0896
  • eISSN : 1464-3391
  • Web of Science ID : WOS:000476649000009

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