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European Journal of Nuclear Medicine and Molecular Imaging
Published in: European Journal of Nuclear Medicine and Molecular Imaging 3/2011

01-03-2011 | Short Communication

In vivo imaging of neuroinflammation in the rodent brain with [11C]SSR180575, a novel indoleacetamide radioligand of the translocator protein (18 kDa)

Authors: Fabien Chauveau, Hervé Boutin, Nadja Van Camp, Cyrille Thominiaux, Philippe Hantraye, Luc Rivron, Frank Marguet, Marie-Noëlle Castel, Thomas Rooney, Jesus Benavides, Frédéric Dollé, Bertrand Tavitian

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 3/2011

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Abstract

Purpose

Neuroinflammation is involved in neurological disorders through the activation of microglial cells. Imaging of neuroinflammation with radioligands for the translocator protein (18 kDa) (TSPO) could prove to be an attractive biomarker for disease diagnosis and therapeutic evaluation. The indoleacetamide-derived 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, SSR180575, is a selective high-affinity TSPO ligand in human and rodents with neuroprotective effects.

Methods

Here we report the radiolabelling of SSR180575 with 11C and in vitro and in vivo imaging in an acute model of neuroinflammation in rats.

Results

The image contrast and the binding of [11C]SSR180575 are higher than that obtained with the isoquinoline-based TSPO radioligand, [11C]PK11195. Competition studies demonstrate that [11C]SSR180575 has high specific binding for the TSPO.

Conclusion

[11C]SSR180575 is the first PET radioligand for the TSPO based on an indoleacetamide scaffold designed for imaging neuroinflammation in animal models and in the clinic.
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Metadata
Title
In vivo imaging of neuroinflammation in the rodent brain with [11C]SSR180575, a novel indoleacetamide radioligand of the translocator protein (18 kDa)
Authors
Fabien Chauveau
Hervé Boutin
Nadja Van Camp
Cyrille Thominiaux
Philippe Hantraye
Luc Rivron
Frank Marguet
Marie-Noëlle Castel
Thomas Rooney
Jesus Benavides
Frédéric Dollé
Bertrand Tavitian
Publication date
01-03-2011
Publisher
Springer-Verlag
Published in
European Journal of Nuclear Medicine and Molecular Imaging / Issue 3/2011
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-010-1628-5

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