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European Journal of Nuclear Medicine and Molecular Imaging

Published in:

01-03-2008

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

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

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Special Issue 1/2008

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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Title: Development and evaluation of compounds for imaging of β-amyloid plaque by means of positron emission tomography
Authors: Gjermund Henriksen
Behrooz H. Yousefi
Alexander Drzezga
Hans-Jürgen Wester
Publication date: 01-03-2008
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue Special Issue 1/2008
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-007-0705-x

At a glance: The STEP trials

Springer Medicine

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

Abstract

Purpose

Methods

Results

Conclusion

At a glance: The STEP trials

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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