Comparative myocardial uptake characteristics of hexakis (alkylisonitrile) technetium(I) complexes. Effect of lipophilicity.
Comparative myocardial uptake characteristics of hexakis (alkylisonitrile) technetium(I) complexes. Effect of lipophilicity.
复制标题
六基（烷基异腈）锝（I）复合物的比较心肌摄取特性。
DOI：
10.1097/00004424-198901000-00007
复制
发表时间：
1989
影响因子：
6.7
通讯作者：
Jones,AG
中科院分区：
文献类型：
--
作者：
Piwnica-Worms,D;Kronauge,JF;Holman,BL;Davison,A;Jones,AG
六（烷基异腈）锝 (I) 复合物是一类新型阳离子、亲脂性心肌灌注显像剂。为了进一步评估亲脂性对心肌摄取特性的影响，作者系统地合成并测试了细胞和整个动物系统中不同亲脂性的 Tc-异腈复合物。在单层培养的鸡心脏细胞中，细胞平台水平摄取通常与复合物的亲脂性（通过反相高效液相色谱测定）（r=.71）以及成像兔心脏的闪烁照相强度相关（r=.91）。这一趋势的例外情况表明，其他因素，例如复合物的大小和末端烷基链支化的形式也可能影响吸收。数据表明，亲脂性和单独的阳离子电荷都不足以预测心肌摄取。此外，将复合物静脉注射到兔子体内，使用中等亲脂性的试剂显示出最佳的心肌图像。结果表明，静脉内给药后，低亲脂性的复合物由于心脏细胞摄取低而产生次优的心肌图像，而高亲脂性的复合物由于与其他器官和室的过度结合而产生相对较差的心肌可视化。
Hexakis (alkylisonitrile) technetium (I) complexes are a new class of cationic, lipophilic myocardial perfusion imaging agents. To further evaluate the effect of lipophilicity on myocardial uptake characteristics, the authors systematically synthesized and tested Tc-isonitrile complexes of varying lipophilicity in both cellular and whole animal systems. In chick heart cells in monolayer culture, cellular plateau level uptake in general correlated with lipophilicity of the complexes (determined by reverse phase high performance liquid chromatography)(r=. 71) as well as with scintigraphic intensity of imaged rabbit hearts (r=. 91). Exceptions to this trend indicated that additional factors such as size of the complex and form of the terminal alkyl chain branching also may have influenced uptake. The data indicated that neither the lipophilic properties nor the cation charge alone were sufficient to predict myocardial uptake. In addition, intravenous injection of complexes into rabbits showed optimal myocardial images with agents of intermediate lipophilicity. Results indicated that, following intravenous administration, complexes of low lipophilicity yielded suboptimal myocardial images because of low heart cell uptake, whereas complexes of high lipophilicity yielded poor relative myocardial visualization because of excessive binding to additional organs and compartments.