Design, synthesis and preliminary evaluation of 18F-labelled 1,8-naphthyridin- and quinolin-2-one-3-carboxamide derivatives for PET imaging of CB2 cannabinoid receptor

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dc.contributor.authorSaccomanni, Gen_AU
dc.contributor.authorPascali, Gen_AU
dc.contributor.authorDel Carlo, Sen_AU
dc.contributor.authorPanetta, Den_AU
dc.contributor.authorDe Simone, Men_AU
dc.contributor.authorBertini, Sen_AU
dc.contributor.authorBurchielli, Sen_AU
dc.contributor.authorDigiacomo, Men_AU
dc.contributor.authorMacchia, Men_AU
dc.contributor.authorManera, Cen_AU
dc.contributor.authorSalvadori, PAen_AU
dc.date.accessioned2020-03-24T00:29:20Zen_AU
dc.date.available2020-03-24T00:29:20Zen_AU
dc.date.issued2015-06-15en_AU
dc.description.abstractIn the present work, we report the synthesis of new aryliodonium salts used as precursors of single-stage nucleophilic 18F radiofluorination. The corresponding unlabelled fluorinated derivatives showed to be CB2 cannabinoid receptor specific ligands, with Ki values in the low nanomolar range and high CB2/CB1 selectivity. The radiolabelled compound [18F]CB91, was successfully formulated for in vivo administration, and its preliminary biodistribution was assessed with microPET/CT. This tracer presented a reasonable in vivo stability and a preferential extraction in the tissues that constitutionally express CB2 cannabinoid receptor. The results obtained indicate [18F]CB91 as a possible candidate marker of CB2 cannabinoid receptor distribution. This study would open the way to further validation of this tracer for assessing pathologies for which the expression of this receptor is modified. © 2015 by Elsevier Ltd.en_AU
dc.identifier.citationSaccomanni, G., Pascali, G., Del Carlo, S., Panetta, D., De Simone, M., Bertini, S., Burchielli, S., Digiacomo, M., Macchia, M., Manera, C. & Salvadori, P. A. (2015). Design, synthesis and preliminary evaluation of 18 F-labelled 1, 8-naphthyridin-and quinolin-2-one-3-carboxamide derivatives for PET imaging of CB2 cannabinoid receptor. Bioorganic & Medicinal Chemistry Letters, 25(12), 2532-2535. doi:10.1016/j.bmcl.2015.04.055en_AU
dc.identifier.govdoc8874en_AU
dc.identifier.issn0960-894Xen_AU
dc.identifier.issue12en_AU
dc.identifier.journaltitleBioorganic & Medicinal Chemistry Lettersen_AU
dc.identifier.pagination2532-2535en_AU
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2015.04.055en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9210en_AU
dc.identifier.volume25en_AU
dc.language.isoenen_AU
dc.publisherElsevieren_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectReceptorsen_AU
dc.subjectIn vivoen_AU
dc.subjectFluorine 18en_AU
dc.subjectCT-guided radiotherapyen_AU
dc.subjectRadiopharmaceuticalsen_AU
dc.titleDesign, synthesis and preliminary evaluation of 18F-labelled 1,8-naphthyridin- and quinolin-2-one-3-carboxamide derivatives for PET imaging of CB2 cannabinoid receptoren_AU
dc.typeJournal Articleen_AU
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