Development and evaluation of compounds for imaging of β-amyloid plaque by means of positron emission tomography

  • Gjermund Henriksen
  • Behrooz H. Yousefi
  • Alexander Drzezga
  • Hans-Jürgen Wester
Article

Abstract

Purpose

The proof of concept for in vivo targeting of β-amyloid plaques (Aβ) in patients with Alzheimer’s disease (AD) by means of nuclear imaging methods has been shown in recent clinical studies.

Methods

For positron emission tomography (PET), the five compounds [11C]PIB, 3′[18F]FPIB, [18F]FDDNP, [11C]SB-13 and [18F]F-SB-13 have been developed by a formal charge neutralisation of agents used for staining of AD brain post mortem.

Results

In AD-patients, these compounds have been shown to possess a selective uptake in the brain regions known to have a high Aβ-load. Progress towards tracers with proportionality between tracer uptake and quantity of Aβ-load, of use for longitudinal studies of AD patients, is addressed in the current development of Aβ-tracers.

Conclusion

Despite the extensive information on the structure–affinity relationship of several Aβ-binding compounds, data on the regional brain binding kinetics—beyond uptake in healthy rodents—have been obtained only for a few compounds. Recent results indicate that PET-imaging of Aβ-deposits in transgenic rodent models of AD is feasible which may be valuable for a more relevant preclinical evaluation of Aβ-tracers.

Keywords

Alzheimer’s disease Amyloid plaque Nuclear imaging PET SPECT 

Abbreviations

NFTs

neurofibrillary tangles

FTLD

frontotemporal lobar degeneration

PSP

progressive supranuclear palsy

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Copyright information

© Springer-Verlag 2007

Authors and Affiliations

  • Gjermund Henriksen
    • 1
  • Behrooz H. Yousefi
    • 1
  • Alexander Drzezga
    • 1
  • Hans-Jürgen Wester
    • 1
  1. 1.Department of Nuclear Medicine, Klinikum rechts der IsarTechnische Universität MünchenMünchenGermany

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