α-Aryl substituted GdDOTA derivatives, the perfect contrast agents for MRI?
α-Aryl substituted GdDOTA derivatives, the perfect contrast agents for MRI?
复制标题
DOI：
10.1039/d3cc05989h
复制
发表时间：
2024-01-09
影响因子：
4.9
通讯作者：
Woods，Mark
中科院分区：
文献类型：
--
作者：
Maier，Karley B.;Rust，Lauren N.;Woods，Mark
增强Gd3+螯合物作为核磁共振松驰剂的性能，有可能降低剂量，提高安全性，并减轻对我们地表水的环境影响。三十多年来对操纵Gd3+性质的研究未能开发出一种同时优化所有相关参数并提供最大弛豫度的螯合物。将芳基取代基引入GdDOTA螯合物的悬臂的α位置，首次提供了同时优化所有物理化学性质的螯合物。通过与人血清白蛋白结合来减缓翻滚，松弛系数为110mM−1 S−1，接近可能的最大值。作为离散的螯合物，这些α-芳基取代的GdDOTA螯合物表现出比目前使用的试剂高2-3倍的松弛活性，即使在现代临床核磁共振使用的更高的磁场(1.5T和3.0T)下也是如此。
Enhancing the performance of Gd3+ chelates as relaxation agents for MRI has the potential to lower doses, improving safety and mitigating the environmental impact on our surface waters. More than three decades of research into manipulating the properties of Gd3+ have failed to develop a chelate that simultaneously optimizes all relevant parameters and affords maximal relaxivity. Introducing aryl substituents into the α-position of the pendant arms of a GdDOTA chelate affords chelates that, for the first time, simultaneously optimize all physico-chemical properties. Slowing tumbling by binding to human serum albumin affords a relaxivity of 110 ± 5 mM−1 s−1, close to the maximum possible. As discrete chelates, these α-aryl substituted GdDOTA chelates exhibit relaxivities that are 2–3 times higher than those of currently used agents, even at the higher fields (1.5 & 3.0 T) used in modern clinical MRI.