Synthesis of biphenyltrienes as probes for beta-amyloid plaques

J Med Chem. 2006 May 4;49(9):2841-4. doi: 10.1021/jm051020k.


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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / diagnosis*
  • Alzheimer Disease / metabolism
  • Alzheimer Disease / pathology
  • Amyloid beta-Peptides / metabolism*
  • Brain / metabolism*
  • Brain / pathology
  • Humans
  • Ligands
  • Molecular Probes / analysis*
  • Molecular Probes / chemical synthesis*
  • Molecular Probes / chemistry
  • Molecular Probes / metabolism
  • Molecular Structure
  • Plaque, Amyloid / metabolism*
  • Plaque, Amyloid / pathology


  • Amyloid beta-Peptides
  • Ligands
  • Molecular Probes