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Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging 1/2008

01.03.2008

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

verfasst von: Gjermund Henriksen, Behrooz H. Yousefi, Alexander Drzezga, Hans-Jürgen Wester

Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging | Sonderheft 1/2008

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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.
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Metadaten
Titel
Development and evaluation of compounds for imaging of β-amyloid plaque by means of positron emission tomography
verfasst von
Gjermund Henriksen
Behrooz H. Yousefi
Alexander Drzezga
Hans-Jürgen Wester
Publikationsdatum
01.03.2008
Verlag
Springer-Verlag
Erschienen in
European Journal of Nuclear Medicine and Molecular Imaging / Ausgabe Sonderheft 1/2008
Print ISSN: 1619-7070
Elektronische ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-007-0705-x

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