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

Jintaek Kim, Fumihiko Yamamoto, Satoru Karasawa, Takahiro Mukai, Minoru Maeda

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4 Citations (Scopus)

Abstract

An ascorbate analog labeled with iodine-131, 6-deoxy- 6-[ 131I]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 [131I]iodide in 2-pentanone at 130-140°C. HPLC purification using a reversephase column gave 6-deoxy-6-[131I]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 14C-labeled ascorbic acid and 6-deoxy-6-[18F]fluoro-L-ascorbic acid, in spite of high level of deiodination.

Original languageEnglish
Pages (from-to)366-371
Number of pages6
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume52
Issue number9
DOIs
Publication statusPublished - Jul 2009

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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