PET Radioligands for In Vivo Visualization of Neuroinflammation

ISSN: 1873-4286 (Online)
ISSN: 1381-6128 (Print)

Volume 22, 46 Issues, 2016

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PET Radioligands for In Vivo Visualization of Neuroinflammation

Current Pharmaceutical Design, 20(37): 5897-5913.

Author(s): Dieter Ory, Sofie Celen, Alfons Verbruggen and Guy Bormans.

Affiliation: Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.


Neuroinflammation is a well-orchestrated, dynamic, multicellular process playing a major role in neurodegenerative disorders. The microglia which make up the innate immune system of the central nervous system are key cellular mediators of neuroinflammatory processes. In normal condition they exert a protective function, providing tissue repair by releasing anti-inflammatory cytokines and neurotrophic factors. Upon neuronal injury or infection, they become overactivated, thereby releasing neurotoxic substances, amplifying neuroinflammation leading to neurodegeneration. Positron emission tomography (PET) provides a sensitive non-invasive imaging technique to study and quantify receptor and enzyme expression. A radiolabeled tracer for a protein (over)expressed in neuroinflammation and more specifically for the overactivated microglia would be useful as a diagnostic tool in the follow-up of neuroinflammation progression and to study the efficacy of anti-inflammatory therapy over time. In this manuscript, an overview of potential PET tracer targets upregulated during neuroinflammation is provided together with the current radiotracers used to image these targets. In addition, lead structures to develop radiotracers for new targets are suggested.


Neuroinflammation, positron emission tomography.

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Article Details

Volume: 20
Issue Number: 37
First Page: 5897
Last Page: 5913
Page Count: 17
DOI: 10.2174/1381612820666140613120212

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