Radiosynthesis, in vivo biological evaluation, and imaging of brain lesions with [123I]-CLINME, a new SPECT tracer for the translocator protein

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dc.contributor.authorMattner, Fen_AU
dc.contributor.authorQuinlivan, Men_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorPham, TQen_AU
dc.contributor.authorLiu, Xen_AU
dc.contributor.authorJackson, TWen_AU
dc.contributor.authorBerghofer, PJen_AU
dc.contributor.authorFookes, CJRen_AU
dc.contributor.authorDikic, Ben_AU
dc.contributor.authorGrégoire, MCen_AU
dc.contributor.authorDollé, Fen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.date.accessioned2020-03-29T23:37:53Zen_AU
dc.date.available2020-03-29T23:37:53Zen_AU
dc.date.issued2015-06-25en_AU
dc.date.statistics2020-03-20en_AU
dc.description.abstractThe high affinity translocator protein (TSPO) ligand 6-chloro-2-(4′-iodophenyl)-3-(N,N-methylethyl)imidazo[1,2-a]pyridine-3-acetamide (CLINME) was radiolabelled with iodine-123 and assessed for its sensitivity for the TSPO in rodents. Moreover neuroinflammatory changes on a unilateral excitotoxic lesion rat model were detected using SPECT imaging. [123I]-CLINME was prepared in 70–80% radiochemical yield. The uptake of [123I]-CLINME was evaluated in rats by biodistribution, competition, and metabolite studies. The unilateral excitotoxic lesion was performed by injection of α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid unilaterally into the striatum. The striatum lesion was confirmed and correlated with TSPO expression in astrocytes and activated microglia by immunohistochemistry and autoradiography. In vivo studies with [123I]-CLINME indicated a biodistribution pattern consistent with TPSO distribution and the competition studies with PK11195 and Ro 5-4864 showed that [123I]-CLINME is selective for this site. The metabolite study showed that the extractable radioactivity was unchanged [123I]-CLINME in organs which expresses TSPO. SPECT/CT imaging on the unilateral excitotoxic lesion indicated that the mean ratio uptake in striatum (lesion : nonlesion) was 2.2. Moreover, TSPO changes observed by SPECT imaging were confirmed by immunofluorescence, immunochemistry, and autoradiography. These results indicated that [123I]-CLINME is a promising candidate for the quantification and visualization of TPSO expression in activated astroglia using SPECT. © 2015 F. Mattner et al.en_AU
dc.identifier.articlenumber729698en_AU
dc.identifier.citationMattner, F., Quinlivan, M., Greguric, I., Pham, T., Liu, X., Jackson, T., Berghofer, P., Fookes, C. J. R., Dikic, B., Grégoire, M. C., Dollé, F. & Katsifis, A. (2015). Radiosynthesis, in vivo biological evaluation, and imaging of brain Lesions with [123I]-CLINME, a new SPECT tracer for the translocator protein. Disease Markers, 2015, 729698. doi:10.1155/2015/729698en_AU
dc.identifier.govdoc8810en_AU
dc.identifier.issn1875-8630en_AU
dc.identifier.journaltitleDisease Markersen_AU
dc.identifier.urihttp://dx.doi.org/10.1155/2015/729698en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9298en_AU
dc.identifier.volume2015en_AU
dc.language.isoenen_AU
dc.publisherHindawi Publishing Corporationen_AU
dc.subjectIn vivoen_AU
dc.subjectBrainen_AU
dc.subjectProteinsen_AU
dc.subjectSingle photon emission computed tomographyen_AU
dc.subjectTranslocationen_AU
dc.subjectRatsen_AU
dc.subjectReceptorsen_AU
dc.titleRadiosynthesis, in vivo biological evaluation, and imaging of brain lesions with [123I]-CLINME, a new SPECT tracer for the translocator proteinen_AU
dc.typeJournal Articleen_AU
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