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DEVELOPMENT OF RADIOPHARMACEUTICALS BASED ON THE BIOCHEMICAL FUNCTIONS OF ASCORBIC ACID

Research Project

Project/Area Number 03453150
Research Category

Grant-in-Aid for General Scientific Research (B)

Allocation TypeSingle-year Grants
Research Field Radiation science
Research InstitutionKYUSHU UNIVERSITY

Principal Investigator

MAEDA Minoru  KYUSHU UNIVERSITY, FACULTY OF PHARMACEUTICAL SCIENCES, PROFESSOR, 薬学部, 教授 (70101178)

Project Period (FY) 1991 – 1992
Project Status Completed (Fiscal Year 1992)
Budget Amount *help
¥3,800,000 (Direct Cost: ¥3,800,000)
Fiscal Year 1992: ¥1,200,000 (Direct Cost: ¥1,200,000)
Fiscal Year 1991: ¥2,600,000 (Direct Cost: ¥2,600,000)
KeywordsL-ascorbic acid / 6-deoxy-6-[^<18>F]fluoro-L-ascorbic acid / fluorine-18 / tissue distribution / brain ischemia / radiopharmaceutical / 6-デオキシ-6-〔F-18〕フルオロ-L-アスコルビン酸 / フッ素-18 / 脳虚血ラット / Lーアスコルビン酸 / フルオロアスコルビン酸 / 腫瘍
Research Abstract

A one-pot synthesis of 6-deoxy-6-[^<18>F]fluoro-L-ascorbic acid (^<18>F-DFA) has been developed via nucleophilic displacement of a cyclic sulfate with [^<18>F]- fluoride ion in 15% radiochemical yield. Tissue distribution studies with ^<18>F-DFA in rats showed high uptake of radioactivity in the adrenals, kidneys and liver-organs known to have high concentration of L-ascorbic acid. The slow and low uptake of activity in the brain was observed between 10 and 120 min after i.v. injection. In vivo behavior of ^<18>F-DFA in mice bearing 3- methylcholanthrene-induced fibrosarcoma, and in rats bearing transplanted RG-C6 tumor in brain demonstrated its ability to accumulate in the tumors. Comparison of tissue accumulation of ^<18>F-DFA in normal rats and ascorbic acid deficient ODS rats indicated that endogenous ascorbic acid in rats does not affect the in vivo behavior of ^<18>F-DFA.
Regional brain distribution of ^<18>F-DFA was investigated by using in vivo model of cerebral ischemia. Global ischemia was induced in rats by cutting arteiae vertebralis, and then occluding carotid arteries with a microvascular clamp for 20 min. Increased uptake of radioactivity in the cerebral cortex, hypothalamus and amygdala followed by injection of ^<18>F-DFA was observed at 5 days after the termination of the ischemic period. This finding suggests that ^<18>F-DFA may play an important role in repair mechanism of neural injury after cerebral ischemia. Thus, ^<18>F-DFA seemingly has a great potential as a brain radiopharmaceutical based on the biochemical functions of L-ascorbic acid for positron emission tomography.

Report

(3 results)
  • 1992 Annual Research Report   Final Research Report Summary
  • 1991 Annual Research Report
  • Research Products

    (4 results)

All Other

All Publications (4 results)

  • [Publications] 山本 文彦,佐々木 茂貴,前田 稔: "Positron Labeled Antioxidants:Synthesis and Tissue Biodistribution of 6-Deoxy-6-[ ^<18>F]fluoro-L-ascorbic Acid" Appl.Radiat.Isot.43. 633-639 (1992)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1992 Final Research Report Summary
  • [Publications] R. YAMAMOTO, S. SASAKI and M. MAEDA: "Positron Labeled Antioxidants:Synthesis and Tissue Biodistribution of 6-deoxy-6-[F-18]fluoro-L-ascorbic acid" Appl. Radiat. Isot.Vol.43, No.5. 633-639 (1992)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1992 Final Research Report Summary
  • [Publications] 山本 文彦,佐々木 茂貴,前田 稔: "Positron Labeled Antioxidants:Synthesis and Tissue Biodistribution of 6-Deoxy-6〔^<18>F〕fluoro-L-ascorbic Acid" Appl.Radiat.Isot.43. 633-639 (1992)

    • Related Report
      1992 Annual Research Report
  • [Publications] 山本 文彦,佐々木 茂貴,前田 稔: "Positron Labeled Analogs of Antioxidants:Synthesis and Tissue Biodistribution of 6ーDeoxyー6ー〔 ^<18>F〕fluoroーLーascorbic Acid" Appl.Radiat.Isotopes. 43. (1992)

    • Related Report
      1991 Annual Research Report

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Published: 1991-04-01   Modified: 2016-04-21  

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