title: Synthesis and biodistribution of a Lipophilic 64Cu-labeled monocationic Copper(II) complex.
abstract: The lipophilic, monocationic copper(II) complex of the diiminedioxime ligand 2,10-di-n-butyl-3,9-dimethyl-1,4,8,11-tetraazaundeca-1,3,8,10-tetraen-1,11-dione dioxime was synthesized and labeled with 64Cu. The biological properties of the 64Cu-labeled complex were measured in vivo and in vitro. In vivo, the complex shows uptake by the heart similar to that of 99mTc-tetrofosmin. In vitro, its uptake by multidrug resistant and non-resistant MES-SA tumor cells parallels that of 99mTc-MIBI, a well-characterized marker of multidrug resistance. These results suggest that this class of copper complexes may form the basis for the development of a 64Cu PET radiopharmaceutical for the functional imaging of multidrug resistance and/or myocardial perfusion.
authors.affiliation: Division of Nuclear Medicine, Children's Hospital, Boston, MA 02115, USA. alan.packard@tch.harvard.edu
authors.forename: Alan B
authors.initials: AB
authors.lastname: Packard
authors.forename: James F
authors.initials: JF
authors.lastname: Kronauge
authors.forename: Eva
authors.initials: E
authors.lastname: Barbarics
authors.forename: Salma
authors.initials: S
authors.lastname: Kiani
authors.forename: S T
authors.initials: ST
authors.lastname: Treves
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003301:Copper Radioisotopes; D006321:Heart / Q000000981:diagnostic imaging; D006801:Humans; D008024:Ligands; D008297:Male; D009206:Myocardium / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D051381:Rats; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D003301:Copper Radioisotopes; D008024:Ligands; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; C465864:copper(II)-2,10-di-n-butyl-3,9-dimethyl-1,4,8,11-tetraazaundeca-1,3,8,10-tetraen-1,11-dione dioxime