62Cu-labeled bifunctional radiopharmaceuticals with metabolizable ester groups.
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.
Matsumoto
K
K
Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kyoto University, Japan.
Fujibayashi
Y
Y
Arano
Y
Y
Wada
K
K
Yokoyama
A
A
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
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)