Engelstad B L, White D L, Huberty J P, Wynne C S, Ramos E C, McNamara M T, Goldberg H I
Invest Radiol. 1987 Mar;22(3):232-8. doi: 10.1097/00004424-198703000-00009.
A simple method to test new gadolinium complexes potentially useful as enhancement agents for magnetic resonance imaging was developed. Healthy rats underwent scintigraphy with two potential hepatobiliary agents, diethyl IDA and diisopropyl IDA complexed with gadolinium-153. Control products included 153Gd DTPA, 153GdCl3 and technetium-99m diethyl IDA. As shown scintigraphically, 153Gd IDA complexes were partially excreted by urinary and hepatobiliary excretion early after administration. These findings paralleled significant reduction in 1H T1 values of excised livers. However, these agents exhibited prolonged 153Gd whole-body retention. The prolonged tissue distribution of 153Gd activity in animals given 153Gd diethyl IDA did not differ significantly from that observed in animals given GdCl3, and could be attributed to chemical instability or reticuloendothelial uptake. The scintigraphic method permits screening of gadolinium complexes in animals by showing mass balance, kinetics, distribution, and effective stability. Biologic effects of tracer or pharmacologic levels can be compared with those of carrier-free and carrier-added pharmaceuticals.
开发了一种简单的方法来测试可能用作磁共振成像增强剂的新型钆配合物。健康大鼠用两种潜在的肝胆剂进行闪烁扫描，即与钆 - 153络合的二乙基亚氨基二乙酸（diethyl IDA）和二异丙基亚氨基二乙酸（diisopropyl IDA）。对照产品包括钆 - 153二乙三胺五乙酸（153Gd DTPA）、氯化钆 - 153（153GdCl3）和锝 - 99m二乙基亚氨基二乙酸。闪烁扫描显示，给药后早期，钆 - 153 IDA络合物通过尿液和肝胆排泄部分排出。这些发现与切除肝脏的氢质子磁共振成像T1值显著降低相一致。然而，这些药剂表现出钆 - 153在全身的滞留时间延长。给予钆 - 153二乙基亚氨基二乙酸的动物体内钆 - 153活性的组织分布延长与给予氯化钆的动物中观察到的情况没有显著差异，这可能归因于化学不稳定性或网状内皮细胞摄取。闪烁扫描方法通过显示质量平衡、动力学、分布和有效稳定性，允许在动物中筛选钆配合物。示踪剂或药理水平的生物学效应可以与无载体和添加载体的药物的效应进行比较。
