6-[18F]Fluoro-Dehydroascorbic Acid:Synthesis and Tissue Distribution in Mice
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概要
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6-Deoxy-6-[<SUP>18</SUP>F]fluoro-L-threo-2,3-hexodiulosonic acid γ-lactone(6-[<SUP>18</SUP>F]fluoro-dehydroascorbic acid, <SUP>18</SUP>F-FDHA)was synthesized by oxidation of 6-deoxy-6-[<SUP>18</SUP>F]fluoro-L-ascorbic acid(<SUP>18</SUP>F-DFA)with Br<SUB>2</SUB>, a route that is analogous to the original synthesis of FDHA, in order to develop a radiotracer for nuclear medical imaging. Tissue biodistribution of <SUP>18</SUP>F-FDHA in fibrosarcoma-bearing mice showed a low accumulation of radioactivity in the brain, with both substantial in vivo defluorination and low tumoral uptake levels. Several organs of mice unfed for 24h showed a more significant increase in radioactivity postinjection of <SUP>18</SUP>F-FDHA than did fed mice. Co-injection with 2-deoxyglucose of <SUP>18</SUP>F-FDHA did not significantly alter brain and tumor uptake, as confirmed by tissue-to-blood ratios, and as compared to control experiments. Thus, <SUP>18</SUP>F-FDHA does not exhibit desirable properties as a brain-targeting imaging agent for ascorbic acid bioactivity.
- 公益社団法人 日本アイソトープ協会の論文
公益社団法人 日本アイソトープ協会 | 論文
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