Evaluation of CLINDE as potent translocator protein (18 kDa) SPECT radiotracer reflecting the degree of neuroinflammation in a rat model of microglial activation

Abstract

These results demonstrate that CLINDE is suitable for TSPO in vivo SPECT imaging to explore their involvement in neurodegenerative disorders associated with microglial activation.

Evaluation of Prion Deposits and Microglial Activation in Scrapie-Infected Mice Using Molecular Imaging Probes

“…A number of new alternative radioligands are therefore currently being developed worldwide to improve the specificity of the signal, including iodinated CLINDE, a highly promising iodinated TSPO tracer [13,14,25]. With the aim of proposing in vivo scintigraphic explorations for the diagnosis and/or follow-up of prion disease by SPECT imaging, we performed ex vivo experiments in the same animal model using two iodinated tracers, i.e.…”

“…This ligand can be radiolabelled with 123 I in order to apply it for the detection of neuroinflammation using SPECT imaging. Using a rat model of brain excitotoxic lesions, we recently demonstrated that in vivo accumulation of CLINDE accurately and specifically reflected the changing degree of neuroinflammation [14]. As the cerebral PrP sc deposits are closely associated with a chronic inflammatory response dominated by microglial activation, we hypothesized that CLINDE could be used to detect the microglial activation in TSE brains.…”

Mephedrone in Adolescent Rats: Residual Memory Impairment and Acute but Not Lasting 5-HT Depletion

“…The ligand [ 125 I]CLINDE [38], [39] was used to quantify levels of translocator protein (TSPO) in rats repeatedly exposed to MMC or METH. TSPO receptors display upregulation with neurodegeneration, concurrent with the microglial activation observed during neuroinflammatory processes [40].…”

Comparison of in vivo binding properties of the 18-kDa translocator protein (TSPO) ligands [18F]PBR102 and [18F]PBR111 in a model of excitotoxin-induced neuroinflammation

“…As in previous studies, neuroinflammation was investigated 7 days after treatment. [31,32,[34][35][36]. Striatal neurons exhibit an enhanced vulnerability to the oxidative damage and the resultant inflammatory response is induced by excitotoxic processes resulting from strong activation of NMDA and AMPA glutamate receptors [36].…”

“…Initial ligands such as [ 11 C]PK11195 show significant specificity, but a less favourable signal-to-noise ratio, attributed to high nonspecific binding, reducing the effectiveness of this tracer for detecting subtle changes in neuroinflammation. The unilateral striatal excitotoxicity model for induction of consistent and reproducible neuroinflammation has been used extensively for screening the in vivo properties of radiotracers targeting the TSPO [12,19,[31][32][33][34]. As in previous studies, neuroinflammation was investigated 7 days after treatment.…”