Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains.

Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains. Research Abstract Details 

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Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains. Abstract Text:

Masahiro Ono,Mamoru Haratake,Hiroshi Mori,Morio Nakayama,Masahiro Ono,Mamoru Haratake,Hiroshi Mori,Morio Nakayama,

A novel series of chalcone derivatives for in vivo imaging beta-amyloid plaques in the brain of Alzheimer's disease (AD) were synthesized and characterized. When in vitro binding studies using Abeta aggregates were carried out with chalcone derivatives, the binding affinities for Abeta aggregate varied from 3 to 105 nM. The radioiodinated chalcones were successfully prepared through an iododestannylation reaction from the corresponding tributyltin derivatives using hydrogen peroxide as the oxidant in high yields and with high radiochemical purities. Biodistribution studies in normal mice after iv injection of the radioiodinated chalcones displayed high brain uptake (2.0-4.7% ID/g at 2 min) and rapid clearance from the brain (0.2-0.6% ID/g at 30 min), which is highly desirable for amyloid imaging agents. The results in this study suggest that the novel radioiodinated chalcones may be useful amyloid imaging agents for detecting beta-amyloid plaques in the brain of AD.

Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains. Publishing Authors By Initials

M Ono,M Haratake,H Mori,M Nakayama,M Ono,M Haratake,H Mori,M Nakayama,

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Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 6802-9

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 21

MONTH: 08

YEAR: 2007

Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Novel chalcones as probes for in vivo imaging of beta-amyloid plaques in Alzheimer's brains.

AFFILIATION: Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-Machi, Nagasaki, Japan. mono@nagasaki-u.ac.jp

Country: England

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MEDLINETA: Bioorg Med Chem

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