Styryl-based compounds as potential in vivo imaging agents for beta-amyloid plaques

Chembiochem. 2007 Sep 24;8(14):1679-87. doi: 10.1002/cbic.200700154.

Abstract

A group of styryl-based neutral compounds has been synthesized in this study for potential use as in vivo imaging agents for beta-amyloid plaques. Of 56 candidates, 14 compounds were found to label beta-amyloid plaques well on Alzheimer's disease (AD) human brain sections in vitro. The binding affinity to beta-amyloid fibrils was then determined by measuring the change in fluorescence intensity. Interestingly, we found that a class of quinaldine-styryl scaffold compounds displays specific binding to beta-amyloid fibrils. A representative compound, STB-8, was used in ex vivo and in vivo imaging experiments on an AD transgenic mouse model and demonstrated excellent blood-brain barrier (BBB) permeability and specific staining of the AD beta-amyloid plaques.

Publication types

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

MeSH terms

  • Alzheimer Disease / diagnosis*
  • Alzheimer Disease / metabolism*
  • Amyloid beta-Peptides / chemistry*
  • Animals
  • Blood-Brain Barrier
  • Contrast Media / pharmacology*
  • Humans
  • Kinetics
  • Mice
  • Mice, Transgenic
  • Microscopy, Fluorescence / methods
  • Models, Chemical
  • Permeability
  • Plaque, Amyloid / pathology*
  • Protein Binding
  • Spectrometry, Fluorescence / methods

Substances

  • Amyloid beta-Peptides
  • Contrast Media