~(99)Tc~mN-MIBI 的制备及其生物分布研究

  • 摘要: 为获得新型心肌显像剂,以SnCl2·2H2O为还原剂制备了99Tcm≡N2+中间体,然后由配体交换反应得到标记率>90%的99TcmN-MIBI配合物,并优化了配体交换反应条件。99TcmN-MIBI在制备后室温放置10h放化纯度仍>90%,分配系数P=33.70。小鼠体内生物分布结果显示:99TcmN-MIBI具有较高的早期心肌摄取,清除较快,在注射后5min时心/血、心/肺、心/肝比分别为3.18、1.72和1.42。其与99Tcm-MIBI的生物分布有显著不同,可望用于早期心肌显像

     

    Abstract: THE PREPARATION AND BIODISTRIBUTION OF A NEW 99TcmNITRIDO COMPLEX 99TcmNMIBIZhang Xianzhong\ Wang Xuebin\ Zhang Junbo (Department of Chemistry, Beijing Normal University, 100875)ABSTRACTThe technetium99m nitrido intermediate is synthesized by using SnCl2·2H2O as reductant, and the complex 99TcmNMIBI is obtained through ligandexchange reaction. The labelling yield of 99TcmNMIBI is over 95% by TLC. The conditions of preparing 99TcmNMIBI are optimized. Results of stability and partition coefficient of 99TcmNMIBI indicate that the complex is lipophilic and stable over 10 h at room temperature. The biodistribution of 99TcmNMIBI in mice shows high myocardium uptake, and rather rapid clearance. For 5min postinjection the hearttoblood, hearttolung and hearttoliver ratios are 3.18, 1.72 and 1.42, respectively. The new complex may be suitable for instant myocardial imaging. 99TcmNMIBI has significant different biodistribution characteristics from 99TcmMIBI. Based on these promising properties, 99TcmNMIBI should be a new potential myocardial perfusion imaging agent.Key words myocardial perfusion imaging agent 99TcmN core radiopharmaceutical biodistribution 99TcmNMIBI

     

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