Zhang Junbo, Guo Haixun, Zhang Shijian, Lin Yan, Wang Xuebin
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5168-70. doi: 10.1016/j.bmcl.2008.08.109. Epub 2008 Sep 3.
The ciprofloxacin dithiocarbamate (CPFXDTC) was synthesized and radiolabeled with (99m)TcN intermediate to form the (99m)TcN-CPFXDTC complex in high yield (>95%). No decomposition of the complex at room temperature was observed over a period of 6 h. Its partition coefficient indicated that it was a good lipophilic complex. The bacterial binding assay studies showed (99m)TcN-CPFXDTC had a better binding affinity as compared with (99m)Tc-ciprofloxacin. Biodistribution results in induced infection mice showed (99m)TcN-CPFXDTC had higher uptake at the sites of infection and better abscess/blood ratio than that of (99m)Tc-ciprofloxacin, suggesting (99m)TcN-CPFXDTC would be a novel potential infection imaging agent.
合成了环丙沙星二硫代氨基甲酸盐（CPFXDTC），并用(99m)TcN中间体进行放射性标记，以高产率（>95%）形成(99m)TcN-CPFXDTC络合物。在室温下6小时内未观察到该络合物的分解。其分配系数表明它是一种良好的亲脂性络合物。细菌结合试验研究表明，与(99m)Tc-环丙沙星相比，(99m)TcN-CPFXDTC具有更好的结合亲和力。在诱导感染小鼠中的生物分布结果表明，(99m)TcN-CPFXDTC在感染部位的摄取更高，脓肿/血液比值比(99m)Tc-环丙沙星更好，表明(99m)TcN-CPFXDTC将是一种新型的潜在感染显像剂。
