2013 Fiscal Year Final Research Report
Development of PET molecular probes for imaging alpha-synuclein in the brain
| Project/Area Number |
23659605
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Radiation science
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| Research Institution | Tokyo Metropolitan Geriatric Hospital and Institute of Gerontology |
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Principal Investigator |
TOYOHARA Jun 地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 専門副部長 (50425659)
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| Co-Investigator(Renkei-kenkyūsha) |
ISHIWATA Kiichi 地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究部長 (50143037)
SAKATA Muneyuki 地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究員 (00403329)
ISHII Kenji 地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究部長 (10231135)
ODA Keiichi 地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究員 (70224235)
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| Project Period (FY) |
2011 – 2013
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| Keywords | 放射性医薬品・造影剤 |
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| Research Abstract |
Five phenothiazine and a polyphenol derivatives were radiolabeled as potential PET molecular imaging probes for alpha-synuclein imaging in the brain. The four of five phenothiazine derivatives were successfully radiolabeled by 11C-methyl iodide or 11C-methyl triflate in a good yield with high specific activity. Dedicated small animal PET imaging showed these phenothiazine derivatives crossed the blood-brain barrier (BBB) with rapid washout from the brain. Another one-phenothiazine and polyphenol derivatives did not cross the BBB.
In conclusion, our initial studies suggested that phenothiazine derivatives are good candidate for in vivo imaging of alpha-synuclein aggregation in the brain. Further structural optimizations of these compounds are needed.
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Research Products
(10 results)
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[Presentation] Synthesis and evaluation of a fluorine-18-labeled 7α-(3-fluoropropyl)estradiol2013
Author(s)
Okamoto, M., Matsui, A., Kitagawa, Y., Toyohara, J., Ishiwata, K., Yoshimoto, M. and Shimizu, I
Place of Presentation
Jeju
Year and Date
20130512-17
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