Synthesis and evaluation of radioiodinated ligands for the study of peripheral benzodiazepine receptors using SPECT

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dc.contributor.authorKatsifis, Aen_AU
dc.contributor.authorMattner, Fen_AU
dc.contributor.authorMardon, Ken_AU
dc.contributor.authorDikic, Ben_AU
dc.contributor.authorPapazian, Ven_AU
dc.contributor.authorGreguric, Ien_AU
dc.date.accessioned2023-01-30T03:29:45Zen_AU
dc.date.available2023-01-30T03:29:45Zen_AU
dc.date.issued2002-04-29en_AU
dc.date.statistics2022-02-02en_AU
dc.description.abstractThe peripheral benzodiazepine receptor (PBR) is a multimeric protein complex located in the outer mitochondrial membrane and predominantly found in steroid producing organs and glial cells in the brain. The PBR have been implicated in the control of cell proliferation and differentiation and shown to display increased levels in a variety of malignant tumours and neurodegenerative disorders. A series of potent imidazo[1,2-a]pyridines have been prepared for development as radiopharmaceuticals to study these disorders in patients using nuclear medicine imaging techniques. In vitro studies indicate that compounds substituted with an electronegative atom in the 6 position of the pyridine ring, a lipophilic group or halogen in the 4'-position of the 2-phenyl ring, and lower alkyl methyl or ethyl substituents on the amide nitrogens of the side chain, exhibit high affinity and selective binding. ' N'N'-dimethyl- and the N'N'-diethyl 6-chloro-(4'-iodophenyl)imidazo[1,2-a]pyridine-3-acetamide 1 and 2 displayed optimum in vitro properties and were thus selected for radiolabelling with the diagnostic radionuclide iodine-123. Radioiodination was achieved by iododestannylation of the corresponding tributyl stannane precursor in the presence of peracetic acid. Purification by C-18 reverse phase HPLC gave the desired products in 70-80% radiochemical yields and in greater than 98% radiochemical purity. Biodistribution studies in normal rodents indicated high uptake of radioactivity in tissues with known PBR sites. Preliminary imaging studies in rodents bearing mammary adenocarcinomas indicated high uptake in the tumour with retention of activity after 24 h. The synthesis, structure activity studies, radiolabelling and biological studies of these compounds will be presented.en_AU
dc.identifier.booktitleFrance-Australia Symposium on nuclear medicine : methodology, clinical applications and pharmacology : volume of proceedings, Monday 29th April 2002, Sheraton on the park, Sydney, Australiaen_AU
dc.identifier.citationKatsifis, A., Mattner, F., Mardon, K., Dikic, B., Papazian, V., & Greguric, I. (2002). Synthesis and evaluation of radioiodinated ligands for the study of peripheral benzodiazepine receptors using SPECT. Poster presented to the France-Australia Symposium on nuclear medicine : methodology, clinical applications and pharmacology : volume of proceedings, Sheraton on the Park, Sydney, Australia, Monday 29th April 2002. Lucas Heights, NSW : Australian Nuclear Science and Technology Organisation, (pp. 63).en_AU
dc.identifier.conferencenameFrance-Australia Symposium on nuclear medicine : methodology, clinical applications and pharmacologyen_AU
dc.identifier.conferenceplaceSydney, Australiaen_AU
dc.identifier.conferencestartdate29 April 2002en_AU
dc.identifier.editorsAustralian Nuclear Science and Technology Organisationen_AU
dc.identifier.pagination63en_AU
dc.identifier.placeofpublicationLucas Heights, NSWen_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/14570en_AU
dc.language.isoenen_AU
dc.publisherAustralian Nuclear Science and Technology Organisationen_AU
dc.subjectBiological accumulationen_AU
dc.subjectImidazolesen_AU
dc.subjectIodine 123en_AU
dc.subjectNervous system diseasesen_AU
dc.subjectOrganic iodine compoundsen_AU
dc.subjectPyridinesen_AU
dc.subjectRadiochemical analysisen_AU
dc.subjectRadiopharmaceuticalsen_AU
dc.subjectReceptorsen_AU
dc.subjectSingle photon emission computed tomographyen_AU
dc.subjectSynthesisen_AU
dc.titleSynthesis and evaluation of radioiodinated ligands for the study of peripheral benzodiazepine receptors using SPECTen_AU
dc.typeConference Posteren_AU
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