中文摘要：

为拓展脱氧葡萄糖（DG）在肿瘤代谢显像中的应用,以新型核素64Cu标记葡萄糖胺-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸（DOTA-DG）.通过优化反应条件,于25℃反应30 min后得到高放化纯度和高比活度的标记化合物64 Cu-DOTA-DG,标记产物经放射性高效液相色谱（ Radio-HPLC）检测.体外稳定性实验结果表明,64 Cu-DOTA-DG有良好的稳定性.将64 Cu-DOTA-DG通过尾静脉注射入荷瘤肝癌细胞（ Hep-G2）裸鼠体内,分别于注射后1和3 h进行小动物正电子发射断层扫描（ Micro-PET）显像.结果表明,其在肿瘤部位有所富集.64 Cu-DOTA-DG的合成及分子显像研究拓宽了以18 F-氟代脱氧葡萄糖为代表的肿瘤代谢类显像剂的应用范围,为新型核素标记肿瘤代谢显像剂提供一种新途径.

英文摘要：

2-（4-Isothiocyanatobenzyl）-1,4,7,10-tetraazacyclo-dodecane-1,4,7,10-tetraacetic acid-D-glucose （ DOTA-DG） was synthesized and radiolabeled with 64 Cu. The DOTA-DG dissolved in sodium acetate buffer （pH=5. 5） was added to the eluent of64Cu. The solution was stirred and placed at 25℃ for 30 min. The la-beling efficiency and radiochemical purity of 64 Cu-DOTA-DG were all over 95%, as determined by radio-HPLC. The in vitro stability of the conjugates was analyzed in 0.1 mol/L PBS and 0.1 mol/L NaAc and it showed excellent in vitro stability. 14. 8 MBq of64 Cu-DOTA-DG was injected to Hep-G2 xenograft models via tale vein. Positron emission tomography images were taken 1 and 3 h after the injection. These images sugges-ted that there was high tumor uptake of 64 Cu-DOTA-DG. The results suggested that 64 Cu-DOTA-DG could provide images much clearer than the DG labeled with 99m Tc, 111 In and 68 Ga, and observation of the metabo-lism of DG much longer. These preliminary data show that 64 Cu-DOTA-DG appears to be useful in PET ima-ging.