Short Communication

European Journal of Nuclear Medicine and Molecular Imaging

, Volume 38, Issue 3, pp 509-514

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

  • Fabien ChauveauAffiliated withService Hospitalier Frédéric Joliot, CEA, DSV, I²BMINSERM U1023, Université Paris SudCreatis; CNRS UMR 5220; INSERM U630; INSA Lyon, Université Lyon 1
  • , Hervé BoutinAffiliated withService Hospitalier Frédéric Joliot, CEA, DSV, I²BMINSERM U1023, Université Paris SudFaculty of Life Sciences, University of Manchester
  • , Nadja Van CampAffiliated withService Hospitalier Frédéric Joliot, CEA, DSV, I²BMINSERM U1023, Université Paris Sud
  • , Cyrille ThominiauxAffiliated withService Hospitalier Frédéric Joliot, CEA, DSV, I²BM
  • , Philippe HantrayeAffiliated withMIRCEN, CEA, DSV, I²BM
  • , Luc RivronAffiliated withGMPK-Global Isotope Chemistry and Metabolite Synthesis Department (ICMS), Sanofi-Aventis
  • , Frank MarguetAffiliated withCNS Department, Sanofi-Aventis
  • , Marie-Noëlle CastelAffiliated withCNS Department, Sanofi-Aventis
  • , Thomas RooneyAffiliated withCNS Department, Sanofi-Aventis
    • , Jesus BenavidesAffiliated withCNS Department, Sanofi-Aventis
    • , Frédéric DolléAffiliated withService Hospitalier Frédéric Joliot, CEA, DSV, I²BM
    • , Bertrand TavitianAffiliated withService Hospitalier Frédéric Joliot, CEA, DSV, I²BMINSERM U1023, Université Paris Sud Email author 

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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.

Keywords

Translocator protein (18 kDa) Peripheral benzodiazepine receptor Neuroinflammation 11C-SSR180575 11C-PK11195