1990 Fiscal Year Final Research Report Summary
Development of Biologically Active Nucleosides Labeled with Positron Emitting ^<18>F
| Project/Area Number |
01571193
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Research Field |
Biological pharmacy
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| Research Institution | Tohoku University |
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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)
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| 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)
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| Project Period (FY) |
1989 – 1990
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| Keywords | F-18 / Br-75 / Fuluorodeoxyuridine / Bromodeoxyuridine / Tumor Diagnosis / Nucleoside / Nucleic Acid Metabolism / Positron Emission Tomography |
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| 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.
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Research Products
(5 results)
