A Single-Pot Template Reaction Towards a Manganese-Based T 1 Contrast Agent
A Single-Pot Template Reaction Towards a Manganese-Based T 1 Contrast Agent
复制标题
锰基 T 1 造影剂的单锅模板反应
DOI：
10.1002/ange.202100885
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发表时间：
2021
影响因子：
--
通讯作者：
Anbu S
中科院分区：
文献类型：
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作者：
Anbu S
锰基造影剂（MnCA）已成为钆基造影剂（GdCA）的合适替代品。然而，由于其动力学不稳定性和费力的合成程序，只有少数MnCA获得了临床MRI应用。在这项工作中，我们采用了一种高度创新的单锅模板合成策略来开发MnCA，MnLMe，并在体外研究了最重要的物理化学性质。MnLMe在中等（20和64 MHz）和高磁场（300和400 MHz）下显示出最佳的r1弛豫率，并在与BSA结合时（Ka=4.2×103M−1）增强r1b =21.1mM−1s−1（20 MHz，298 K，pH 7.4）。 体内研究表明，MnLMe通过肾脏排泄被完整地清除到膀胱中，并且与市售GdCA Magnevist相比具有延长的血液半衰期。MnLMe显示出作为新型MRI造影剂的巨大前景。
Manganese‐based contrast agents (MnCAs) have emerged as suitable alternatives to gadolinium‐based contrast agents (GdCAs). However, due to their kinetic lability and laborious synthetic procedures, only a few MnCAs have found clinical MRI application. In this work, we have employed a highly innovative single‐pot template synthetic strategy to develop a MnCA,MnLMe, and studied the most important physicochemical properties in vitro.MnLMedisplays optimizedr1relaxivities at both medium (20 and 64 MHz) and high magnetic fields (300 and 400 MHz) and an enhancedr1b=21.1 mM−1s−1(20 MHz, 298 K, pH 7.4) upon binding to BSA (Ka=4.2×103M−1). In vivo studies show thatMnLMeis cleared intact into the bladder through renal excretion and has a prolonged blood half‐life compared to the commercial GdCA Magnevist.MnLMeshows great promise as a novel MRI contrast agent.