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Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers

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Abstract

Neurodegenerative, inflammatory and neoplastic brain disorders involve neuroinflammatory reactions, and a biomarker of neuroinflammation would be useful for diagnostic, drug development and therapy control of these frequent diseases. In vivo imaging can document the expression of the peripheral benzodiazepine receptor (PBR)/translocator protein 18 kDa (TSPO) that is linked to microglial activation and considered a hallmark of neuroinflammation. The prototype positron emission tomography tracer for PBR, [11C]PK11195, has shown limitations that until now have slowed the clinical applications of PBR imaging. In recent years, dozens of new PET and SPECT radioligands for the PBR have been radiolabelled, and several have been evaluated in imaging protocols. Here we review the new PBR ligands proposed as challengers of [11C]PK11195, critically analyze preclinical imaging studies and discuss their potential as neuroinflammation imaging agents.

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Acknowledgements

We wish to thank all our excellent colleagues with whom we had exciting discussions during the TOPIM’07 “Imaging neuroinflammation” meeting in Les Houches (February 2007) and the 5th French Australian symposium on Nuclear medicine (November 2007), with a special emphasis for our continuous dialogue with Pr. Michael Kassiou and the many fruitful discussions with Prs. Andrew Katsifis and Denis Guilloteau. Work in our laboratory is funded by the EMIL and DIMI European networks of excellence. NVC is the recipient of a FWO fellowship from Belgium.

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  1. CEA, Institut d’Imagerie BioMédicale, Service Hospitalier Frédéric Joliot, Laboratoire d’Imagerie Moléculaire Expérimentale, Orsay, France

    Fabien Chauveau, Nadja Van Camp, Frédéric Dollé & Bertrand Tavitian

  2. INSERM, U803, Orsay, France

    Fabien Chauveau, Nadja Van Camp & Bertrand Tavitian

  3. Faculty of Life Sciences, University of Manchester, Manchester, M13 9PT, UK

    Hervé Boutin

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  1. Fabien Chauveau
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Correspondence to Bertrand Tavitian.

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Chauveau, F., Boutin, H., Van Camp, N. et al. Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers. Eur J Nucl Med Mol Imaging 35, 2304–2319 (2008). https://doi.org/10.1007/s00259-008-0908-9

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