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 |
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Format: | Artikel |
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. |
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ISSN: | 1433-7851 1521-3773 |
DOI: | 10.1002/anie.202100885 |