<br>MRI 造影剂的化学：当前挑战和新领域。,Chemical Reviews

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MRI 造影剂的化学：当前挑战和新领域。
Chemical Reviews ( IF 51.4 ) Pub Date : 2018-10-16 , DOI: 10.1021/acs.chemrev.8b00363
Jessica Wahsner ₁ , Eric M Gale ₁ , Aurora Rodríguez-Rodríguez ₁ , Peter Caravan ₁

Affiliation

全世界每年进行数千万次对比增强磁共振成像 (MRI) 检查。提高诊断准确性的造影剂几乎都是小型亲水性钆（III）基螯合物。近年来，人们对这些化合物的长期安全性产生了担忧，这刺激了对替代品的研究。人们还致力于开发新的分子靶向造影剂或可以感知局部环境病理变化的试剂。这篇全面的综述描述了临床批准的造影剂的最新技术、其作用机制以及影响其安全性的因素。在此基础上，我们描述了生成 MR 图像对比度的不同机制，例如弛豫、化学交换饱和转移和直接检测，以及对这些目的有效的分子类型。接下来，我们描述了通过提高弛豫率、提高对金属离子释放的抵抗力或通过转向不含钆 (III) 的替代品来制造更安全的造影剂的努力。最后，我们调查了通过直接生化靶向或通过设计响应性或可激活造影剂使造影剂对病理学更具特异性的方法。

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Chemistry of MRI Contrast Agents: Current Challenges and New Frontiers.

Tens of millions of contrast-enhanced magnetic resonance imaging (MRI) exams are performed annually around the world. The contrast agents, which improve diagnostic accuracy, are almost exclusively small, hydrophilic gadolinium(III) based chelates. In recent years concerns have arisen surrounding the long-term safety of these compounds, and this has spurred research into alternatives. There has also been a push to develop new molecularly targeted contrast agents or agents that can sense pathological changes in the local environment. This comprehensive review describes the state of the art of clinically approved contrast agents, their mechanism of action, and factors influencing their safety. From there we describe different mechanisms of generating MR image contrast such as relaxation, chemical exchange saturation transfer, and direct detection and the types of molecules that are effective for these purposes. Next we describe efforts to make safer contrast agents either by increasing relaxivity, increasing resistance to metal ion release, or by moving to gadolinium(III)-free alternatives. Finally we survey approaches to make contrast agents more specific for pathology either by direct biochemical targeting or by the design of responsive or activatable contrast agents.

更新日期：2018-10-16

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