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

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European Journal of Nuclear Medicine and Molecular Imaging Aims and scope Submit manuscript

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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Abbreviations

NFTs:

neurofibrillary tangles

FTLD:

frontotemporal lobar degeneration

PSP:

progressive supranuclear palsy

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Conflict of interest statement

There are no conflicts of interest for any of the authors.

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Authors and Affiliations

  1. Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaningerstrasse 22, 81675, München, Germany

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

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  1. Gjermund Henriksen
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  2. Behrooz H. Yousefi
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  3. Alexander Drzezga
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  4. Hans-Jürgen Wester
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Correspondence to Gjermund Henriksen.

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Henriksen, G., Yousefi, B.H., Drzezga, A. et al. Development and evaluation of compounds for imaging of β-amyloid plaque by means of positron emission tomography. Eur J Nucl Med Mol Imaging 35 (Suppl 1), 75–81 (2008). https://doi.org/10.1007/s00259-007-0705-x

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