Organometallic Chemistry - Volume 43
Organometallic Chemistry - Volume 43
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有机金属化学 - 第 43 卷
DOI：
10.1039/9781788017077-00083
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发表时间：
2020
期刊：
影响因子：
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通讯作者：
Brito B
中科院分区：
文献类型：
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作者：
Brito B
自从钆螯合物被引入临床以来，它已经成为产生对比增强MRI的不可或缺的工具。许多钆造影剂（GdCA）已成功应用于临床，但最近由于安全性问题，其中一些造影剂受到限制。大环GdCA已被证明是高度稳定的，并具有良好的安全记录;该GdCA设计提供了一个模板，用于开发具有更高弛豫率的新试剂。本章探讨了生产高弛豫率，高稳定性GdCA的重要设计考虑因素，并检查了一些最近的例子，已经经历了临床试验。这些实施例集中于增加GdCA的分子量以减缓在溶液中的翻滚的不同方法，这改善了弛豫性，同时保留了高稳定性螯合物核。通过水分子的缔合进一步增加GdCA的分子量的亲水臂的掺入已被证明在该目标中是有效的，并且不会显著影响GdCA的生物分布。
Gadolinium chelates have become an indispensable tool for the production of contrast enhanced MRI since their introduction into the clinic. A number of gadolinium contrast agents (GdCAs) have been successfully translated into the clinic, however recently some of these have been restricted due to safety concerns. The macrocyclic GdCAs have been shown to be highly stable and have a good safety record; this GdCA design provides a template for the development of new agents with higher relaxivity. This chapter explores the important design considerations for the production of high relaxivity, high stability GdCAs and examines some recent examples that have undergone clinical trials. These examples focus on different methods of increasing the molecular weight of the GdCA to slow tumbling in solution, which improves relaxivity whilst retaining the high stability chelate core. The incorporation of hydrophilic arms that further increase the molecular weight of the GdCA through association of water molecules has been shown to be effective in this goal and does not significantly impact upon the biodistribution of the GdCA.