Research for novel ^<18>F-labeled radiopharmaceuticals prepared by [^<18>F]fluoromethylation.
| Project/Area Number |
16390332
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Radiation science
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| Research Institution | Tohoku University |
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Principal Investigator |
IWATA Reni Tohoku University, Cyclotron and Radioisotope Center, Professor, サイクロトロン・ラジオアイソトープセンター, 教授 (60143038)
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| Co-Investigator(Kenkyū-buntansha) |
YANAI Kazuhiko Tohoku University, Graduate School of Medicine, Professor, 大学院医学系研究科, 教授 (50192787)
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| Project Period (FY) |
2004 – 2006
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| Project Status |
Completed (Fiscal Year 2006)
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| Budget Amount *help |
¥13,600,000 (Direct Cost: ¥13,600,000)
Fiscal Year 2006: ¥2,700,000 (Direct Cost: ¥2,700,000)
Fiscal Year 2005: ¥6,200,000 (Direct Cost: ¥6,200,000)
Fiscal Year 2004: ¥4,700,000 (Direct Cost: ¥4,700,000)
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| Keywords | PET / F-18 / radiopharmaceutical / Molecular probe / Automated synthesis / Fluoromethyl |
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| Research Abstract |
The objectives of this research project was to prepare a variety of 18F-labeled compounds using [^<18>F]fluoromethyl bromide or [^<18>F]fluoromethyl triflate and evaluate their usefulness in PET diagnosis. The main subjects were (1)automated synthesis of [^<18>F]fluoromethyl triflate, (2)synthetic use in the preparation of ^<18>F-labeled radiopharmaceuticals, (3)development of automated module for preparation of [^<18>F]fluorocholine, and (4)biological/clinical evaluation of [^<18>F]fluoromethyltyrosine.
1.An automated miniature module for the preparation of [^<18>F]fluoromethyl bromide from [^<18>F]fluoride was successfully developed using the original manifold technology.
2.[^<18>F]Fluoromethylation was carried out on various compounds using [^<18>F]fluoromethyl triflate. It was found, however, that they were all unstable except for [^<18>F]fluorocholine and [^<18>F]fluoromethyltyrosine.
3.An automated miniature module was also developed for the preparation of [^<18>F]fluorocholine using [^<18>F]fluoromethyl triflate.
4.[^<18>F]Fluoromethyltyrosine was evaluated to image tumors and to distinguish them from inflammation. It was shown that [^<18>F]fluoromethyltyrosine was as good a candidate as [^<18>F]fluoromethyltyrosine for imaging tumors.
In conclusion, the usefulness of [^<18>F]fluoromethyl triflate for [^<18>F]Fluoromethylation in convenient preparation of ^<18>F-labeled radiopharmaceuticals was investigated and the results were obtained that many [^<18>F]fluoromethylated compounds were not stable and only [^<18>F]fluorocholine and [^<18>F]fluoromethyltyrosine were stably prepared. They were prepared with the dedicated automated modules and used in basic studies for their evaluation as tumor imaging agents.
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Report
(4 results)
Research Products
(42 results)
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[Journal Article] Initial evaluation of dynamic human imaging using ^<18>F-FRP170 as a new PET tracer for imaging hypoxia.2007
Author(s)
K.Kaneta, Y.Takai, R.Iwata, T.Hakamatsuka, H.Yasuda, K.Nakayama, Y.Ishikawa, S.Watanuki, S.Furumoto, Y.Funaki, E.Nakata, K.Jingu, M.Tsujitani, M.Itoh, H.Fukuda, S.Takahashi, S.Yamada.
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Journal Title
Ann. Nucl. Med. 21
Pages: 101-107
NAID
Description
「研究成果報告書概要(和文)」より
Related Report
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[Journal Article] Initial evaluation of dynamic human imaging using ^<18>F-FRP170 as a new PET tracer for imaging hypoxia.2007
Author(s)
K.Kaneta, Y.Takai, R.Iwata, T.Hakamatsuka, H.Yasuda, K.Nakayama, Y.Ishikawa, S.Watanuki, S.Furumoto, Y.Funaki, E.Nakata, K.Jingu, M.Tsujitani, M.Itoh, H.Fukuda, S.Takahashi, S.Yamada
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Journal Title
Ann.Nucl.Med. 21
Pages: 101-107
NAID
Description
「研究成果報告書概要(欧文)」より
Related Report
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[Journal Article] Initial evaluation of dynamic human imaging using ^<18>F-FRP170 as a new PET tracer for imaging hypoxia.2007
Author(s)
K.Kaneta, Y.Takai, R.Iwata, T.Hakamatsuka, H.Yasuda, K.Nakayama, Y.Ishikawa, S.Watanuki, S.Furumoto, Y.Funaki, E.Nakata, K.Jingu, M.Tsujitani, M.Itoh, H.Fukuda, S.Takahashi, S.Yamada
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Journal Title
Ann. Nucl. Med. 21
Pages: 101-107
NAID
Related Report
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[Journal Article] A PET study of histamine H1 receptors in schizophrenic patients assessed by [^<11>C] doxepin2005
Author(s)
K.Iwabuchi, C.Ito, M.Tashiro, H.Mochizuki, M.Kato, M.Kano, K.Ishii, K.Ishiwata, M.Itoh, R.Iwata, H.Matsuoka, M.Sato, K.Yanai.
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Journal Title
Eur.Neuropsychopharmacol. 15
Pages: 185-191
Related Report
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[Journal Article] Central effeicts of fexofenadine and cetirizine : measurement of psychomotor performance, subjective sleepiness, and brain histamine H_1-receptor occupancy using ^<11>C-doxepin positron emission tomography2004
Author(s)
M.Tashiro, Y.Sakurada, K.Iwabuchi, H.Mochizuki, M.Kato, M.Aoki, Y.Funaki, M.Itoh, R.Iwata, D.F.Wong, K.Yanai
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Journal Title
J. Clinic. Pharmacol 44
Pages: 890-900
Description
「研究成果報告書概要(和文)」より
Related Report
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[Journal Article] Central effects of fexofenadine and cetirizine : measurement of psychomotor performance, subjective sleepiness, and brain histamine H_1-receptor occupancy using ^<11>C-doxepin positron emission tomography.2004
Author(s)
M.Tashiro, Y.Sakurada, K.Iwabuchi, H.Mochizuki, M.Kato, M.Aoki, Y.Funaki, M.Itoh, R.Iwata, D.F.Wong, K.Yanai
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Journal Title
J.Clinic.Pharmacol. 44
Pages: 890-900
Description
「研究成果報告書概要(欧文)」より
Related Report
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[Journal Article] Central effects of fexofenadine and cetirizine : measurement of psychomotor performance, subjective sleepiness, and brain histamine H_1-receptor occupancy using ^<11>C-doxepin positron emission tomography2004
Author(s)
M.Tashiro, Y.Sakurada, K.Iwabuchi, H.Mochizuki, M.Kato, M.Aoki, Y.Funaki, M.Itoh, R.Iwata, D.F.Wong, K.Yanai
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Journal Title
J.Clinic.Pharmacol 44
Pages: 890-900
Related Report
