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

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.

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

Starting from 99mTcO4]- and at a pressure of 0.1 MPa, the important starting material99mTc(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.