In vivo imaging of brain lesions with [11C]CLINME, a new PET radioligand of peripheral benzodiazepine receptors

dc.contributor.authorBoutin, Hen_AU
dc.contributor.authorChauveau, Fen_AU
dc.contributor.authorThominiaux, Cen_AU
dc.contributor.authorKuhnast, Ben_AU
dc.contributor.authorGrégoire, MCen_AU
dc.contributor.authorJan, Sen_AU
dc.contributor.authorTrebossen, Ren_AU
dc.contributor.authorDollé, Fen_AU
dc.contributor.authorTavitian, Ben_AU
dc.contributor.authorMattner, Fen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.date.accessioned2020-02-14T00:06:19Zen_AU
dc.date.available2020-02-14T00:06:19Zen_AU
dc.date.issued2007-08-06en_AU
dc.date.statistics2019-11-21en_AU
dc.description.abstractThe peripheral benzodiazepine receptor (PBR) is expressed by microglial cells in many neuropathologies involving neuroinflammation. PK11195, the reference compound for PBR, is used for positron emission tomography (PET) imaging but has a limited capacity to quantify PBR expression. Here we describe the new PBR ligand CLINME as an alternative to PK11195. In vitro and in vivo imaging properties of [11C]CLINME were studied in a rat model of local acute neuroinflammation, and compared with the reference compound [11C]PK11195, using autoradiography and PET imaging. Immunohistochemistry study was performed to validate the imaging data. [11C]CLINME exhibited a higher contrast between the PBR-expressing lesion site and the intact side of the same rat brain than [11C]PK11195 (2.14 ± 0.09 vs. 1.62 ± 0.05 fold increase, respectively). The difference was due to a lower uptake for [11C]CLINME than for [11C]PK11195 in the non-inflammatory part of the brain in which PBR was not expressed, while uptake levels in the lesion were similar for both tracers. Tracer localization correlated well with that of activated microglial cells, demonstrated by immunohistochemistry and PBR expression detected by autoradiography. Modeling using the simplified tissue reference model showed that R1 was similar for both ligands (R1 ∼ 1), with [11C]CLINME exhibiting a higher binding potential than [11C]PK11195 (1.07 ± 0.30 vs. 0.66 ± 0.15). The results show that [11C]CLINME performs better than [11C]PK11195 in this model. Further studies of this new compound should be carried out to better define its capacity to overcome the limitations of [11C]PK11195 for PBR PET imaging. © 2007 Wiley-Liss, Inc.en_AU
dc.identifier.citationBoutin, H., Chauveau, F., Thominiaux, C., Kuhnast, B., Grégoire, M. C., Jan, S., Trebossen, C., Traitian, B., Mattner, F., & Katsifis., A. (2007). In vivo imaging of brain lesions with [11C] CLINME, a new PET radioligand of peripheral benzodiazepine receptors. GLIA, 55(14), 1459-1468. doi:10.1002/glia.20562en_AU
dc.identifier.govdoc8686en_AU
dc.identifier.issn1098-1136en_AU
dc.identifier.issue14e_AU
dc.identifier.journaltitleGLIAen_AU
dc.identifier.pagination1459-1468en_AU
dc.identifier.urihttp://doi.org/10.1002/glia.20562en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9117en_AU
dc.identifier.volume55en_AU
dc.language.isoenen_AU
dc.publisherJohn Wiley and Sonsen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectInflammationen_AU
dc.subjectReceptorsen_AU
dc.subjectLigandsen_AU
dc.subjectBrainen_AU
dc.subjectRatsen_AU
dc.subjectAutoradiographyen_AU
dc.subjectImagesen_AU
dc.titleIn vivo imaging of brain lesions with [11C]CLINME, a new PET radioligand of peripheral benzodiazepine receptorsen_AU
dc.typeJournal Articleen_AU
Files
License bundle
Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
license.txt
Size:
1.71 KB
Format:
Item-specific license agreed upon to submission
Description:
Collections