2011 Fiscal Year Final Research Report
Development of molecular probe for SPECT imaging of amyloid in the brain
| Project/Area Number |
21390348
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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 | Nagasaki University |
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Principal Investigator |
NAKAYAMA Morio 長崎大学, 大学院・医歯薬学総合研究科, 教授 (60164373)
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| Co-Investigator(Kenkyū-buntansha) |
HARATAKE Mamoru 長崎大学, 大学院・医歯薬学総合研究科, 准教授 (40325668)
ARANO Yasushi 千葉大学, 大学院・薬学研究院, 教授 (90151167)
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| Co-Investigator(Renkei-kenkyūsha) |
ISHIHARA Jyun 長崎大学, 大学院・医歯薬学総合研究科, 准教授 (80250413)
NISHIDA Noriyuki 長崎大学, 大学院・医歯薬学総合研究科, 准教授 (40333520)
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| Project Period (FY) |
2009 – 2011
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| Keywords | アミロイド / アルツハイマー病 / プリオン / SPECT / 分子イメージング |
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| Research Abstract |
We have reported that^<125> I,^<11> C and^<18> F labeled flavonoid derivatives showed excellent characteristics such as high affinity forβ-amyloid(Aβ) aggregates and good uptake into and rapid clearance from the brain. In this study, we have synthesized and evaluated that novel flavonoid derivatives labeled with^<99> mTc that has become the most commonly used radionuclide in diagnostic nuclear medicine. The monoamine-monoamide dithiol(MAMA) and bis-amino-bis-thiol(BAT) were introduced to flavonoid derivatives as chelating site for the formation of stable and lipophilic^<99m> Tc complexes. Some^<99m> Tc-flavonoid derivatives showed high binding affinity for Aβ(1-42) aggregates. In biodistribution experiments using normal mice,^<99m> Tc-BAT-chalcone displayed high uptake in the brain and the radioactivity washed out from the brain rapidly, which is highly desirable for Aβimaging agents
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