Packard Alan B, Kronauge James F, Barbarics Eva, Kiani Salma, Treves S T
Division of Nuclear Medicine, Children's Hospital, Boston, MA 02115, USA.
Nucl Med Biol. 2002 Apr;29(3):289-94. doi: 10.1016/s0969-8051(02)00285-8.
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.
合成了二亚胺二肟配体2,10-二正丁基-3,9-二甲基-1,4,8,11-四氮杂十一碳-1,3,8,10-四烯-1,11-二酮二肟的亲脂性单阳离子铜（II）配合物，并用64Cu进行标记。对64Cu标记的配合物的生物学特性进行了体内和体外测定。在体内，该配合物在心脏中的摄取情况与99mTc-替曲膦相似。在体外，其在多药耐药和非耐药MES-SA肿瘤细胞中的摄取情况与99mTc-MIBI（一种已充分表征的多药耐药标志物）相似。这些结果表明，这类铜配合物可能为开发用于多药耐药和/或心肌灌注功能成像的64Cu PET放射性药物奠定基础。
