[99Tcm(CO)3(CHI)3]+的制备及其生物分布

Preparation and Biodistribution of [99Tcm(Co)3(CHI)3]+

以99TcmO4-淋洗液为起始物,在低压条件下制备了中间体[99Tcm(CO)3(H2O)3]+,并通过配体交换反应得到放化纯度大于90%的[99Tcm(CO)3(CHI)3]+配合物.该配合物在室温下放置6 h以上放化纯度无明显变化.在正常昆明小鼠体内的生物分布实验结果表明,[99Tcm(CO)3(CHI)3]+具有一定的心肌摄取,且滞留也相当好;在注射后5 min和60 min时的心肌摄取值分别为(13.59±2.12)%ID/g和(13.87±1.54)%ID/g.尽管该配合物的肝和肺本底摄取较高,但是与99TcmN-CHI和99Tcm-CHI相比,羰基锝中心核的引入还是大大改善了配合物用于心肌显像的性能,为发展新的心肌显像剂提供了一种新思路.

Starting from [99TcmO4]- and at 0.1 MPa CO pressure conditions, the important starting material [99Tcm(CO)3(H2O3]+ is synthesized. By ligand exchanging of this starting material with isonitrile ligand CHI (Cyclohexylisonitrile), the complex [99Tcm(CO)3(CHI)3]+ is prepared. Its ra-diochemical purity is more than 90%, and it is stable over 6 h at room temperature. The biodistri-bution of this new complex in normal mice indicates that it has some myocardial uptake and maintained well in it, the values of heart uptake at 5 min and 60 min post-injection are (13. 59±2.12)% ID/g and (13. 87±1.54)%ID/g, respectively. Unfortunately the uptakes of non-targets, such as liver and lung, are also quite high. Compared with 99TcmN-CHI and 99Tcm-CHI, the tricarbonyl complex [99Tcm(CO)3(CHI)3]+ has the most suitable properties for myocardial imaging.