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Radiosynthesis and preliminary biodistribution in mice of 6-deoxy-6-[131I]iodo-L-ascorbic acid

✍ Scribed by Jintaek Kim; Fumihiko Yamamoto; Satoru Karasawa; Takahiro Mukai; Minoru Maeda

Publisher: John Wiley and Sons
Year: 2009
Tongue: French
Weight: 216 KB
Volume: 52
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1610

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✦ Synopsis

Abstract

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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