Article Dans Une Revue European Journal of Nuclear Medicine and Molecular Imaging Année : 2010

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

Résumé

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,5trimethyl-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 11 C and in vitro and in vivo imaging in an acute model of neuroinflammation in rats. Results The image contrast and the binding of [ 11 C] SSR180575 are higher than that obtained with the isoquinoline-based TSPO radioligand, [ 11 C]PK11195. Competition studies demonstrate that [ 11 C]SSR180575 has high specific binding for the TSPO. Conclusion [ 11 C]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. Keywords Translocator protein (18 kDa) . Peripheral benzodiazepine receptor . Neuroinflammation . 11 C-SSR180575

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hal-05136842 , version 1 (30-06-2025)

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Fabien Chauveau, Hervé Boutin, Nadja van Camp, Cyrille Thominiaux, Philippe Hantraye, et al.. In vivo imaging of neuroinflammation in the rodent brain with [11C]SSR180575, a novel indoleacetamide radioligand of the translocator protein (18 kDa). European Journal of Nuclear Medicine and Molecular Imaging, 2010, 38, pp.509 - 514. ⟨10.1007/s00259-010-1628-5⟩. ⟨hal-05136842⟩
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