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Synthesis of biphenyltrienes as probes for beta-amyloid plaques.


ABSTRACT: We report a series of p-hydroxy-, p-amino-, p-monomethylamino-, and p-monofluoroethylamino-substituted biphenyltrienes that displayed high binding affinities to beta-amyloid plaques. In an in vitro binding assay using postmortem brain homogenates of Alzheimer's patients and [(125)I]9, the triene compounds showed excellent binding affinities. When labeled with suitable radionuclides, they are useful as in vivo imaging agents for detecting Abeta plaques in the brains of Alzheimer's patients.

SUBMITTER: Zhuang ZP 

PROVIDER: S-EPMC2597440 | biostudies-literature | 2006 May

REPOSITORIES: biostudies-literature

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Synthesis of biphenyltrienes as probes for beta-amyloid plaques.

Zhuang Zhi-Ping ZP   Kung Mei-Ping MP   Kung Hank F HF  

Journal of medicinal chemistry 20060501 9


We report a series of p-hydroxy-, p-amino-, p-monomethylamino-, and p-monofluoroethylamino-substituted biphenyltrienes that displayed high binding affinities to beta-amyloid plaques. In an in vitro binding assay using postmortem brain homogenates of Alzheimer's patients and [(125)I]9, the triene compounds showed excellent binding affinities. When labeled with suitable radionuclides, they are useful as in vivo imaging agents for detecting Abeta plaques in the brains of Alzheimer's patients. ...[more]

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