A single-pot template reaction towards a manganese-based T1 contrast agent

Sellamuthu Anbu, Sabrina H. L. Hoffmann, Fabio Carniato, Lawrence Kenning, Thomas W. Price, Timothy J. Prior, Mauro Botta, Andre F. Martins, Graeme J. Stasiuk

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37 Citations (Scopus)
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Abstract

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 Me, and studied the most important physicochemical properties in vitro. MnL Me 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=4.2×10 3 M −1). In vivo studies show that MnL Me is cleared intact into the bladder through renal excretion and has a prolonged blood half-life compared to the commercial GdCA Magnevist. MnL Me shows great promise as a novel MRI contrast agent.

Original languageEnglish
Pages (from-to)10736-10744
Number of pages9
JournalAngewandte Chemie-International Edition
Volume60
Issue number19
Early online date24 Feb 2021
DOIs
Publication statusPublished - 3 May 2021

Keywords

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

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