Department of Physical Chemistry, Faculty of Science and Technology, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary.
Le Studium, Loire Valley Institute for Advanced Studies, 1 Rue Dupanloup, 45000 Orléans, France.
J Med Chem. 2020 Jun 11;63(11):6057-6065. doi: 10.1021/acs.jmedchem.0c00197. Epub 2020 May 21.
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.
毒性问题促使人们研究用镧系以外的必需金属离子(如 Mn(II))替代基于 Gd(III)的磁共振成像(MRI)造影剂。在此,我们报告了一种大环螯合物 [Mn(PC2A-BP)],它具有高热力学稳定性(log = 14.86,pMn=8.35)和动力学惰性( = 286.2 h),在人血清白蛋白存在下具有出色的弛豫率( = 23.5 mM s,0.49 T,37 °C),使得即使在低剂量(25 μmol/kg)的复合物下,血管的 MRI 信号强度也能显著增加。