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Please use this identifier to cite or link to this item: http://apo.ansto.gov.au/dspace/handle/10238/9298

Title: Radiosynthesis, in vivo biological evaluation, and imaging of brain lesions with [123I]-CLINME, a new SPECT tracer for the translocator protein
Authors: Mattner, F
Quinlivan, M
Greguric, I
Pham, TQ
Liu, X
Jackson, T
Berghofer, PJ
Fookes, CJR
Dikic, B
Gregoire, MC
Dollé, F
Katsifis, A
Keywords: In vivo
Brain
Proteins
Single photon emission tomography
Traslocation
Rats
Receptors
Issue Date: 25-Jun-2015
Publisher: Hindawi Publishing Corporation
Citation: Mattner, F., Quinlivan, M., Greguric, I., Pham, T., Liu, X., Jackson, T., Berghofer, P., Fookes, C. J. R., Dikic, B., Gregoire, 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, 729698. doi:10.1155/2015/729698
Abstract: The 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.
URI: http://dx.doi.org/10.1155/2015/729698
http://apo.ansto.gov.au/dspace/handle/10238/9298
ISSN: 1875-8630
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