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Synthesis of biphenyltrienes as probes for beta-amyloid plaques.

Zhuang ZP, Kung MP, Kung HF

Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

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.

Published 27 April 2006 in J Med Chem, 49(9): 2841-4.
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