4.8 Article

A Single-Pot Template Reaction Towards a Manganese-Based T1 Contrast Agent

期刊

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 60, 期 19, 页码 10736-10744

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202100885

关键词

bishydrated MnCA; blood pool agents; in  vivo MRI; Mn-based contrast agents; template synthesis

资金

  1. RSC Research Fund [RF19-7464]
  2. Swiss Werner Siemens Foundation
  3. Faculty of Medicine at the University of Tuebingen (Nachwuchsgruppen-Programm)
  4. Deutsche Forschungsgemeinschaft (DFG, German Research Foundation) [EXC 2180-390900677]
  5. Universita del Piemonte Orientale
  6. MRC [MR/T002573/1]
  7. MRC [MR/T002573/1] Funding Source: UKRI

向作者/读者索取更多资源

Manganese-based contrast agents have emerged as potential alternatives to gadolinium-based ones, but their clinical application is limited due to synthetic challenges. This study successfully developed a MnCA with optimized relaxivity, MnLMe, through an innovative synthetic strategy, demonstrating promising performance in both in vitro and in vivo studies.
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. MnLMe displays optimized r(1) relaxivities at both medium (20 and 64 MHz) and high magnetic fields (300 and 400 MHz) and an enhanced r(1)(b)=21.1 mM(-1) s(-1) (20 MHz, 298 K, pH 7.4) upon binding to BSA (K-a=4.2x10(3) M-1). In vivo studies show that MnLMe is cleared intact into the bladder through renal excretion and has a prolonged blood half-life compared to the commercial GdCA Magnevist. MnLMe shows great promise as a novel MRI contrast agent.

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