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

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 indo...

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Bibliographic Details
Published in:European journal of nuclear medicine and molecular imaging 2011-03, Vol.38 (3), p.509-514
Main Authors: Chauveau, Fabien, Boutin, Hervé, Van Camp, Nadja, Thominiaux, Cyrille, Hantraye, Philippe, Rivron, Luc, Marguet, Frank, Castel, Marie-Noëlle, Rooney, Thomas, Benavides, Jesus, Dollé, Frédéric, Tavitian, Bertrand
Format: Article
Language:English
Subjects:
Acetamides - metabolism
Animals
Autoradiography
Biomarkers
Brain
Brain - diagnostic imaging
Brain - metabolism
Carbon Radioisotopes
Cardiology
Carrier Proteins - metabolism
Imaging
Indoles - metabolism
Inflammation - diagnostic imaging
Inflammation - metabolism
Inflammation - pathology
Ligands
Medical imaging
Medicine
Medicine & Public Health
Nuclear Medicine
Oncology
Orthopedics
Positron-Emission Tomography - methods
Proteins
Radiochemistry
Radiology
Rats
Receptors, GABA-A - metabolism
Rodents
Short Communication
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Summary: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-4 H -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.
ISSN:1619-7070
1619-7089
DOI:10.1007/s00259-010-1628-5