title: 62Cu-labeled bifunctional radiopharmaceuticals with metabolizable ester groups.
abstract: Generator-produced positron emitting 62Cu-labeled bifunctional radiopharmaceuticals with metabolizable ester groups were synthesized and evaluated for their bifunctionality: the Cu chelating ability and the biochemical reactivity of the ester groups. In vitro studies showed high stability of the Cu chelate site (4,4-dimethyldithiosemicarbazone structure) and enzymatic hydrolysis of the ester site (ethylester or acetylester). The 62Cu-labeled compounds showed in vivo behavior which may be due to their ester hydrolysis.
authors.affiliation: Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Matsumoto
authors.forename: Y
authors.initials: Y
authors.lastname: Fujibayashi
authors.forename: Y
authors.initials: Y
authors.lastname: Arano
authors.forename: K
authors.initials: K
authors.lastname: Wada
authors.forename: A
authors.initials: A
authors.lastname: Yokoyama
mesh_terms: D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis / Q000378:metabolism*; D003301:Copper Radioisotopes / Q000378:metabolism; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000378:metabolism* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D015037:Zinc Radioisotopes
chemical_list: D002614:Chelating Agents; D003301:Copper Radioisotopes; D013882:Thiosemicarbazones; D015037:Zinc Radioisotopes; C074411:acetyl 2,3-dioxopropanal-di-(4,4-dimethylthiosemicarbazone); C074410:ethyl 3,4-dioxobutyrate-di-(4,4-dimethylthiosemicarbazone)