一种新的潜在心肌显像剂[^(99m)Tc(CO)_3(TBI)_3]^+的制备及其生物分布研究  

The Preparation and Biodistribution of a New Potential Myocardial Imaging Agent: Technetium-99m Labeled[Tc(CO)_3(TBI)_3]^+ Complex

作　　者：张现忠[1] 王学斌[1] 温海涛[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《高等学校化学学报》2003年第1期21-24,共4页Chemical Journal of Chinese Universities

基　　金：北京师范大学青年科学基金 (理科 ) (批准号 :10 7195 )资助

摘　　要：以 [99m Tc O4]- 为起始物 ,在 0 .1 MPa下制备了中间体 [99m Tc( CO) 3 ( H2 O) 3 ]+,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 [99m Tc( CO) 3 ( TBI) 3 ]+配合物 .该配合物在室温下放置 6 h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 ,[99m Tc( 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 5 min和 6 0 min后时的心肌摄取值分别为 ( 1 9.0 7± 0 .81 ) % ( ID/g)和 ( 1 8.2 4± 2 .4 1 ) % ( ID/g) .该配合物的非靶本底摄取较低 ,注射 6 0 min后的心 /肝、心 /肺和心 /血摄取比值分别为 1 .0 2 ,5 .83和 2 3.6 9,有望发展为一种新的心肌显像剂 .Starting from [ 99mTcO 4] - and at a pressure of 0.1 MPa, the important starting material[\{ 99mTc(CO) 3\}(H 2O) 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.

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 放射性药物 

分 类 号：R817.42[医药卫生—影像医学与核医学]