The development of the presynaptic cholinergic nerve molecules imaging agent for early diagnosis of Alzheimer's disease
| Project/Area Number |
26293273
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Partial Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Radiation science
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| Research Institution | Kanazawa University |
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Principal Investigator |
Shiba Kazuhiro 金沢大学, 学際科学実験センター, 教授 (40143929)
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| Co-Investigator(Kenkyū-buntansha) |
北村 陽二 金沢大学, 学際科学実験センター, 准教授 (10368483)
小阪 孝史 金沢大学, 学際科学実験センター, 助教 (50579836)
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| Project Period (FY) |
2014-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥16,510,000 (Direct Cost: ¥12,700,000、Indirect Cost: ¥3,810,000)
Fiscal Year 2017: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2016: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2015: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2014: ¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
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| Keywords | アセチルコリントランスポーター / アルツハイマー病 / 早期診断薬 / 分子イメージング / ベサミコール類似体 / アセチルコリントランスポーター(VAChT) / (-)-[11C]OMDV / PET用分子イメージング剤 / ベサミコール類縁体 / PET / アセチルコリントランスポータ / 光学分割 / ベサミコール |
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| Outline of Final Research Achievements |
The purpose of our study is to develop a novel PET imaging agent for early diagnosis of Alzheimer's disease, a severity diagnosis and an effect of treatment judgment. We targeted the acetylcholine transporter(VAChT) which exist in pre-synapse in cholinergic nerve system, which is related to the cognitive impairment of Alzheimer's disease. We newly synthesized (-)-o-[11C]methyl-trans-decalinvesamicol((-)-[11C]OMDV) and o-[77Br]Bromo-trans-decalinvesamicol([77Br]OBDV). (-)-[11C]OMDV and [77Br]OBDV showed a high binding affinity and selectivity for VAChT. In vivo studies demonstrated [11C]OMDV and [77Br]OBDV passage through the blood-brain barrier (BBB) and accumulation in the rat brain. The regional brain distribution of them was accordance with the density distribution of VAChT in brain. These results showed (-)-[11C]OMDV and [77Br]OBDV bound selectively to VAChT in vivo. (-)-[11C]OMDV and [77Br]OBDV was suggested to be useful as a VAChT imaging agent for PET.
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Report
(5 results)
Research Products
(8 results)
