Mn(II)-Based MRI Contrast Agent Candidate for Vascular Imaging

• Published in: Journal of medicinal chemistry Vol. 63; no. 11; pp. 6057 - 6065
• Main Authors: Kálmán, Ferenc K, Nagy, Viktória, Váradi, Balázs, Garda, Zoltán, Molnár, Enikő, Trencsényi, György, Kiss, János, Même, Sandra, Même, William, Tóth, Éva, Tircsó, Gyula
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 11-06-2020
• Subjects: Bioengineering; Imaging; Life Sciences
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/acs.jmedchem.0c00197

Toxicity concerns related to Gd(III)-based magnetic resonance imaging (MRI) agents prompted an intensive research toward their replacement by complexes of essential metal ions, like Mn(II). Here, we report a macrocyclic chelate, [Mn(PC2A-BP)], which possesses high thermodynamic stability (log
= 14.86 and pMn=8.35) and kinetic inertness (
= 286.2 h) as well as as remarkable relaxivity (
= 23.5 mM
s
, 0.49 T, 37 °C) in the presence of human serum albumin, allowing a significant MRI signal intensity increase in the vasculature even at low dose (25 μmol/kg) of the complex.