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Development of Biologically Active Nucleosides Labeled with Positron Emitting ^<18>F

Research Project

Project/Area Number 01571193
Research Category

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

Allocation TypeSingle-year Grants
Research Field Biological pharmacy
Research InstitutionTohoku University

Principal Investigator

ISHIWATA Kiichi  Tohoku Univ., Cyclotron & Radioisotope Center, Research Associate, サイクロトロン・ラジオアイソトープセンター, 助手 (50143037)

Co-Investigator(Kenkyū-buntansha) TAKAHASHI Toshihiro  Tohoku Univ., Cyclotron & Radioisotope Center Research Associate, 助手 (70143039)
IWATA Ren  Tohoku Univ., Cyclotron & Radioisotope Center, Research Associate, 助手 (60143038)
IDO Tatsuo  Tohoku Univ., Cyclotron & Radioisotope Center, Professor, 教授 (80134063)
Project Period (FY) 1989 – 1990
Project Status Completed (Fiscal Year 1990)
Budget Amount *help
¥2,100,000 (Direct Cost: ¥2,100,000)
Fiscal Year 1990: ¥700,000 (Direct Cost: ¥700,000)
Fiscal Year 1989: ¥1,400,000 (Direct Cost: ¥1,400,000)
KeywordsF-18 / Br-75 / Fuluorodeoxyuridine / Bromodeoxyuridine / Tumor Diagnosis / Nucleoside / Nucleic Acid Metabolism / Positron Emission Tomography / フルオロデオキシウリジン / 実験腫瘍 / ^<18>F標識化合物 / 癌診断
Research Abstract

Metabolism of 2-deoxy-5-[^<18>F] fluorouridine (Fdurd), a useful positron emission tomography (PET) tracer of nucleic acid metabolism in tumors, was investigated in tumor-bearing mice and human plasma. Degradation of the tracer in vivo was very rapid. a-[^<18>F] Fluoro-b-alanine (FBAL) wasa main catabolite in the plasma. In tumor tissues, the activated derivatives of FdUrd, FBAL and the other catabolic materials were found; however, contribution of the plasma catabolites to the radioactivity accumulation in the tumor was minor. Nucleic acid metabolism in brain tumors by FdUrd-PET maybe assessed using normal brain regions as a reference.
As new radiopharmaceuticals, 5-[^<75>Br] bromouracil (BrUra) and 5-[^<75>Br]bromo-2'-deoxyuridine (BrdUrd) were prepared from ^<75>Br anion and uracil or 2'-deoxyuridine by a chloramine-T method. The ^<75>Br was prepared by the ^<75>As(^3He,3n)^<75>Br reaction. In tumor-bearing rats given each of the tracer, radioactivity increased in tumor tissues. The level for BrdUrd was 2-times higher than that for BrUra. Although debromination was suggested in vivo, it is expected that the accumulation of the tracer in tumors may correlate with DNA synthesis in the t issue.
As the other compounds, 5-[^<18>F] fluoro-2', 3'-isopropyridine-5'-0-(4-N-acetamide-2, 4-dideoxy-3, 6, 7, 8-tetra-0-acetyl-1-methoxycarbonyl-D-glycero-a-galacto-octapyranosyl) uridine was prepared using [^<18>F]AcOF or [^<18>F]F_2. But, animal studies of the compound was not done. Labeling of adenosine, guanosine and their derivatives using [^<18>F]AcOF and ^<18>F anion has been done unsuccessfully.

Report

(3 results)
  • 1990 Annual Research Report   Final Research Report Summary
  • 1989 Annual Research Report
  • Research Products

    (10 results)

All Other

All Publications (10 results)

  • [Publications] K.Ishiwata,K.Sato,M.Kameyama,et al: "Metabolic fates of 2'ーdeoxyー5〔^<18>F〕fluorouridine in tumorーbearing mice and huma plasma." Nuclear Medicine and Biology. (1991)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1990 Final Research Report Summary
  • [Publications] K.Ishiwata,T.Takahashi,R.Iwata,et al: "Tumor diagnosis by PET:Poteintial of seven tracers examined in five experimental tumors including an artificial metastasis model." Nuclear Medicine and Biology. (1991)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1990 Final Research Report Summary
  • [Publications] K. ISHIWATA, K. SATO, M. KAMEYAMA, T. YOSHIMOTO, T. IDO: "Metabolic Fates of 2'-Deoxy-5-[^<18>F]Fluorouridine in Tumor-Bearing mice and Human Plasma." NUCL. MED. BIOL.(1991)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1990 Final Research Report Summary
  • [Publications] K. ISHIWATA, T. TAKAHSHI, R. IWATA, M. TOMURA, M. TADA, J. ITOH, M. KAMEYAMA, T. IDO: "Tumor Diagnosis by Pet : Potential of Seven Tracers Examined in Five Experimental Tumors Including an Artificial Metastasis Model." NUCL. MED. BIOL.(1991)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1990 Final Research Report Summary
  • [Publications] K. ISHIWATA, ET AL.: "Pharmakokinetics of 2'-Deoxy-5-[^<18>F]Fluorouridine in Human Plasma."

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1990 Final Research Report Summary
  • [Publications] K.Ishiwata,K.Sato,M.Kameyama,et al: "Metabolic fates of 2'ーdeoxyー5ー[ ^<18>F]fluorouridine in tumorーbearing mice and huma plasma." Nuclear Medicine and Biology. (1991)

    • Related Report
      1990 Annual Research Report
  • [Publications] K.Ishiwata,T.Takahashi,R.Iwata,et al: "Tumor diagnosis by PET:Poteintial of seven tracers examined in five experimental tumors including an artificial metastasis model." Nuclear Medicine and Biology. (1991)

    • Related Report
      1990 Annual Research Report
  • [Publications] K.Ishiwata,et al.: "Pharmakokinetics of 2'ーdeoxyー[ ^<18>F]fluorouridine in human plasma."

    • Related Report
      1990 Annual Research Report
  • [Publications] K.Ishiwata et al: "Radiotracers for difterentinl in vivo diagnosis of tumor metabolisms."

    • Related Report
      1989 Annual Research Report
  • [Publications] K.Ishiwata et al: "Pharmacokinetics of 2^'-deoxy-5(^<18>F)fluorouridine in human plasma"

    • Related Report
      1989 Annual Research Report

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Published: 1989-04-01   Modified: 2016-04-21  

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