Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
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.
Zhuang
Zhi-Ping
ZP
Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Kung
Mei-Ping
MP
Kung
Hank F
HF
D000544:Alzheimer Disease / Q000175:diagnosis* / Q000378:metabolism / Q000473:pathology; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D001921:Brain / Q000378:metabolism* / Q000473:pathology; D006801:Humans; D008024:Ligands; D015335:Molecular Probes / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D015394:Molecular Structure; D058225:Plaque, Amyloid / Q000378:metabolism* / Q000473:pathology
D016229:Amyloid beta-Peptides; D008024:Ligands; D015335:Molecular Probes