Burtea Carmen, Laurent Sophie, Colet Jean-Marie, Vander Elst Luce, Muller Robert N
NMR Laboratory, Department of Organic Chemistry, University of Mons-Hainaut, Mons, Belgium.
Invest Radiol. 2003 Jun;38(6):320-33.
A possible approach for the extension of the vascular residence time of contrast agents relies on the renal reabsorption mechanisms of some molecules such as glucose. In this study, various small-molecular-weight glucosyl derivatives of gadolinium diethylenetriaminepentaacetic (Gd-DTPA) were synthesized and their vascular half-life was studied.
Several Gd-DTPA-bisamides carrying glucosyl groups bound by different linkers were prepared. The pharmacokinetics and biodistribution of these compounds were determined on Wistar rats.
The sugar moieties linked to Gd-DTPA efficiently reduce the renal excretion of some derivatives. The interaction with renal carrier has not been clearly demonstrated, nor was any interaction observed with blood components.
Two of the new glucosylated derivatives of Gd-DTPA (Cd-DTPA-BC2-beta-cellobionA 2 and Gd-DTPA-BC4-beta-glucosylA 7) can be proposed as blood-pool MR contrast agents, considering their vascular remanence.
延长造影剂血管驻留时间的一种可能方法依赖于某些分子（如葡萄糖）的肾重吸收机制。在本研究中，合成了钆二乙烯三胺五乙酸（Gd-DTPA）的各种小分子葡萄糖基衍生物，并研究了它们的血管半衰期。
制备了几种带有通过不同连接基连接的葡萄糖基的Gd-DTPA双酰胺。在Wistar大鼠上测定了这些化合物的药代动力学和生物分布。
与Gd-DTPA相连的糖部分有效地减少了某些衍生物的肾排泄。与肾载体的相互作用尚未得到明确证实，与血液成分也未观察到任何相互作用。
考虑到Gd-DTPA的两种新的糖基化衍生物（Gd-DTPA-BC2-β-纤维二糖2和Gd-DTPA-BC4-β-葡萄糖基7）的血管残留情况，可将其作为血池磁共振造影剂。
