Abstract
A stable and inert amphiphilic Mn(II) complex based on a bisamide derivative of 1,4-DO2A (DO2A=tetraazacyclododecane-1,4-diacetic acid) was synthesized and its H-1 NMR relaxometric behavior was investigated as a function of the magnetic field strength, pH and temperature. The interaction with human serum albumin (HSA) was also studied via relaxometry showing a good relaxivity enhancement at low field (at 1T and 298 K the relaxivity increases from 4.5 mM(-1) s(-1) of the Mn(II)-complex to 14.0 mM(-1) s(-1) of the complex-HSA supramolecular adduct). In vivo biodistribution and MRI studies highlighted a rapid and mixed renal/liver elimination without spleen accumulation from healthy mice and good contrast enhancing properties in a breast tumor murine model. A comparison with a clinically approved Gd(III) agent (GdBOPTA, Multihance (R)) underlined that the proposed Mn(II) contrast agent gave comparable tumor contrast enhancement up to 3 hours post-injection.
Lingua originale | Inglese |
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Rivista | ChemMedChem |
Volume | 17 |
Numero di pubblicazione | 24 |
DOI | |
Stato di pubblicazione | Pubblicato - 2022 |
Keywords
- MRI
- Manganese
- contrast agent
- relaxometry
- tumor