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
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- 巻
- 27
- 号
- 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
- ID情報
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- DOI : 10.1016/j.bmc.2019.05.045
- ISSN : 0968-0896
- eISSN : 1464-3391
- Web of Science ID : WOS:000476649000009