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A Single-Pot Template Reaction Towards a Manganese-Based T 1 Contrast Agent.

Sellamuthu AnbuSabrina H L HoffmannFabio CarniatoLawrence KenningThomas W PriceTimothy J PriorMauro BottaAndre F MartinsGraeme J Stasiuk
Published in: Angewandte Chemie (Weinheim an der Bergstrasse, Germany) (2021)
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.
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