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Radiosynthesis and preliminary biodistribution in mice of 6‐deoxy‐6‐[ 131 I]iodo‐ L ‐ascorbic acid
Author(s) -
Kim Jintaek,
Yamamoto Fumihiko,
Karasawa Satoru,
Mukai Takahiro,
Maeda Minoru
Publication year - 2009
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1610
Subject(s) - ascorbic acid , chemistry , radiosynthesis , biodistribution , iodine , radiochemistry , bromine , iodide , in vivo , chromatography , nuclear chemistry , biochemistry , organic chemistry , in vitro , food science , microbiology and biotechnology , biology
An ascorbate analog labeled with iodine‐131, 6‐deoxy‐ 6‐[ 131 I]iodo‐ L ‐ascorbic acid was prepared for evaluation as an in vivo tracer of L ‐ascorbic acid. The no‐carrier‐added radiosynthesis was conducted by nucleophilic bromine–iodine exchange between the brominated precursor and sodium [ 131 I]iodide in 2‐pentanone at 130–140°C. HPLC purification using a reverse‐phase column gave 6‐deoxy‐6‐[ 131 I]iodo‐ L ‐ascorbic acid in radiochemical yield of 36–60% with high radiochemical purity and satisfactory‐specific radioactivity in a total preparation time of 90 min. Biodistribution studies in fibrosarcoma‐bearing mice showed a high uptake in the adrenal glands, accompanied by low activity of tumor accumulation, accumulation properties similar to previous results obtained with 14 C‐labeled ascorbic acid and 6‐deoxy‐6‐[ 18 F]fluoro‐ L ‐ascorbic acid, in spite of high level of deiodination. Copyright © 2009 John Wiley & Sons, Ltd.
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