高等学校化学学报 ›› 2003, Vol. 24 ›› Issue (1): 21.

• 论文 • 上一篇    下一篇

一种新的潜在心肌显像剂[99mTc(CO)3(TBI)3]+的制备及其生物分布研究

张现忠, 王学斌, 温海涛   

  1. 北京师范大学化学系, 北京 100875
  • 收稿日期:2002-04-16 出版日期:2003-01-24 发布日期:2003-01-24
  • 通讯作者: 王学斌(1939年出生),男,教授,博士生导师,主要从事放射性药物化学研究.E-mail:bjsh@bnu.edu.cn E-mail:bjsh@bnu.edu.cn
  • 基金资助:

    北京师范大学青年科学基金(理科)(批准号:107195)资助

The Preparation and Biodistribution of a New Potential Myocardial Imaging Agent: Technetium-99m Labeled[Tc(CO)3(TBI)3]+ Complex

ZHANG Xian-Zhong, WANG Xue-Bin, WEN Hai-Tao   

  1. Department of Chemistry, Beijing Normal University, Beijing 100875, China
  • Received:2002-04-16 Online:2003-01-24 Published:2003-01-24

摘要: 以[99mTcO4]-为起始物,在0.1MPa下制备了中间体[99mTc(CO)3(H2O)1]+,通过配体交换反应,叔丁基异腈(TBI)配体取代该配合物中的3个水分子,制得一种标记率大于90%的[99mTc(CO)1(TBI)1]+配合物.该配合物在室温下放置6h以上,标记率无明显变化.在正常昆明小鼠体内的生物分布实验结果表明,[99mTc(CO)3(TBI)3]+具有较高的心肌摄取,且滞留也相当好,在静脉注射5min和60min后时的心肌摄取值分别为(19.07±0.81)%(ID/g)和(18.24±2.41)%(ID/g).该配合物的非靶本底摄取较低,注射60min后的心/肝、心/肺和心/血摄取比值分别为1.02,5.83和23.69,有望发展为一种新的心肌显像剂.

关键词: 三羰基锝配合物, 心肌显像剂, 叔丁基异腈, 小鼠体内生物分布, 放射性标记

Abstract: Starting from [99mTcO4]- and at a pressure of 0.1 MPa, the important starting material[99mTc(CO)3(H2O)3] + is synthesized. By ligand exchanging of this starting material with isonitrile ligand TBI (t-butyl-isonitrile), the complex [99mTc(CO)3(TBI)3]+ is prepared with a labeling yield higher than 90%, and it is stable over 6 h at room temperature. The biodistribution of this new complex in normal mice indicates that it is well accumulated and maintained in heart. The values of its heart uptake at 5 and 60 min post-injection time are (19.07±0.81)%(ID/g) and (18.24±2.41)%(ID/g), respectively. The uptake ratios of heart to liver, lung, and blood at 60 min post-injection time are 1.02, 5.83 and 23.69, respectively. Its good properties and easy availability make it a very promising myocardial imaging agent.

Key words: Tc(Ⅰ)-carbonyl complex, Myocardial imaging agent, t-Butyl isonitrile(TBI), Biodistribution in mice, Radiolabeling

中图分类号: 

TrendMD: