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

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 innovati...

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Veröffentlicht in:Angewandte Chemie International Edition 2021-05, Vol.60 (19), p.10736-10744
Hauptverfasser: Anbu, Sellamuthu, Hoffmann, Sabrina H L, Carniato, Fabio, Kenning, Lawrence, Price, Thomas W, Prior, Timothy J, Botta, Mauro, Martins, Andre F, Stasiuk, Graeme J
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Sprache:eng
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Zusammenfassung: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.202100885