Browsing by Author "Macchia, M"

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    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
    (Elsevier, 2015-06-15) Saccomanni, G; Pascali, G; Del Carlo, S; Panetta, D; De Simone, M; Bertini, S; Burchielli, S; Digiacomo, M; Macchia, M; Manera, C; Salvadori, PA
    In 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.
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    Identification of chemical byproducts in the radiofluorination of structurally complex aryliodonium salts
    (Springer Nature, 2014-08-24) Pascali, G; Del Carlo, S; Rocchiccioli, S; Signore, G; Saccomanni, G; Manera, C; Macchia, M; Salvadori, PA
    The use of direct radiofluorination of aryliodonium salts represents a promising route to new PET tracers. This study tested the use of these precursors for obtaining candidate ligands of the cannabinoid type-2 receptor. 18F-labelling was performed using microfluidic technology, which allowed obtaining good incorporation yields. A closer inspection of the chemical composition of the reaction mixture evidenced the recurrent occurrence of chemical byproducts (H-adduct) due to a reductive side reaction of these substrates. The H-adduct formation seems to be unrelated to water presence, needed for obtaining a satisfactory incorporation, and may become an important feature for assessing the real-life accessibility of new radiotracers through the use of aryliodonium precursors. © 2014 Akadémiai Kiadó, Budapest, Hungary