Department of Biomedical Sciences, University of Hull, Cottingham Road, Hull, HU6 7RX, UK.
Department of Chemistry, University of Hull, Cottingham Road, Hull, HU6 7RX, UK.
Angew Chem Int Ed Engl. 2021 May 3;60(19):10736-10744. doi: 10.1002/anie.202100885. Epub 2021 Apr 1.
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, MnL , and studied the most important physicochemical properties in vitro. MnL displays optimized r relaxivities at both medium (20 and 64 MHz) and high magnetic fields (300 and 400 MHz) and an enhanced r =21.1 mM s (20 MHz, 298 K, pH 7.4) upon binding to BSA (K =4.2×10 M ). In vivo studies show that MnL is cleared intact into the bladder through renal excretion and has a prolonged blood half-life compared to the commercial GdCA Magnevist. MnL shows great promise as a novel MRI contrast agent.
锰基对比剂（MnCAs）已成为钆基对比剂（GdCAs）的合适替代品。然而，由于其动力学不稳定性和繁琐的合成步骤，只有少数 MnCAs 被应用于临床 MRI。在这项工作中，我们采用了一种极具创新性的单一锅模板合成策略，开发了一种 MnCA，MnL，并对其体外最重要的理化性质进行了研究。MnL 在中（20 和 64MHz）和高磁场（300 和 400MHz）下具有优化的 r 弛豫率，并且在与 BSA 结合后，r = 21.1 mM·s -1（20MHz，298K，pH 7.4）得到增强（K = 4.2×10 M）。体内研究表明，MnL 通过肾脏排泄完整地清除到膀胱中，与商业 GdCA Magnevist 相比，其血液半衰期更长。MnL 有望成为一种新型的 MRI 对比剂。
