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

  • 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
Short Communication

DOI: 10.1007/s00259-010-1628-5

Cite this article as:
Chauveau, F., Boutin, H., Van Camp, N. et al. Eur J Nucl Med Mol Imaging (2011) 38: 509. doi:10.1007/s00259-010-1628-5

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 receptorNeuroinflammation11C-SSR18057511C-PK11195

Copyright information

© Springer-Verlag 2010

Authors and Affiliations

  • Fabien Chauveau
    • 1
    • 2
    • 6
  • Hervé Boutin
    • 1
    • 2
    • 7
  • Nadja Van Camp
    • 1
    • 2
  • Cyrille Thominiaux
    • 1
  • Philippe Hantraye
    • 3
  • Luc Rivron
    • 4
  • Frank Marguet
    • 5
  • Marie-Noëlle Castel
    • 5
  • Thomas Rooney
    • 5
  • Jesus Benavides
    • 5
  • Frédéric Dollé
    • 1
  • Bertrand Tavitian
    • 1
    • 2
  1. 1.Service Hospitalier Frédéric JoliotCEA, DSV, I²BMOrsayFrance
  2. 2.INSERM U1023Université Paris SudOrsayFrance
  3. 3.MIRCENCEA, DSV, I²BMFontenay-aux-RosesFrance
  4. 4.GMPK-Global Isotope Chemistry and Metabolite Synthesis Department (ICMS)Sanofi-AventisParisFrance
  5. 5.CNS DepartmentSanofi-AventisParisFrance
  6. 6.Creatis; CNRS UMR 5220; INSERM U630; INSA LyonUniversité Lyon 1LyonFrance
  7. 7.Faculty of Life SciencesUniversity of ManchesterManchesterUK