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High Relaxivity Mn2+-Based MRI Contrast Agents

机译:高弛豫性基于Mn2 +的MRI造影剂

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摘要

Stable Mn2+ mono-and binuclear complexes containing pentadentate 6,6'-((methylazanediyl)bis(methylene)) dipicolinic acid coordinating units give remarkably high relaxivities due to the presence of two inner-sphere water molecules. The mononuclear derivative binds human serum albumin (HSA) with an association constant of 3372M(-1), which results in the replacement of the coordinated water molecules by donor atoms of protein residues. The dinuclear analogue also binds HSA while leaving one of the Mn2+ centres exposed to the solvent with two coordinated water molecules. Thus, this complex shows remarkably high relaxivities upon protein binding (39.0 mm(-1) s(-1) per Mn, at 20 MHz and 37 degrees C).
机译:含有五齿6,6'-((甲基氮杂二基)双(亚甲基))二吡啶甲酸配位单元的稳定的Mn2 +单核和双核配合物由于存在两个内球水分子而具有显着的高弛豫性。单核衍生物以3372M(-1)的缔合常数结合人血清白蛋白(HSA),从而导致配体水分子被蛋白质残基的供体原子取代。双核类似物还结合HSA,同时使Mn2 +中心之一暴露于带有两个配位水分子的溶剂。因此,该复合物在蛋白质结合后显示出极高的弛豫性(在20 MHz和37摄氏度下,每Mn 39.0 mm(-1)s(-1)/ Mn)。

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