多胺多羧酸双吡哆醇酯顺磁性金属螯合物及其弛豫性能研究

由二乙三胺五乙酸(DTPA)双酸酐和乙二胺四乙酸(EDTA)双酸酐与维生素B₆族化合物吡哆醇(PN)或其衍生物合成了一系列新型的多胺多羧酸双吡哆醇酯衍生物及其钆(Ⅲ)、锰(Ⅱ)、铁(Ⅲ)等顺磁性金属螯合物,研究了其中钆(Ⅲ)和锰(Ⅱ)螯合物在体外水溶液中对水质子的纵向弛豫性能(R₁).结果表明,所有配体和配合物均有很好的水溶性,且对光和空气稳定.螯合物的弛豫率(T₁)可与其母体螯合物相媲美,如钆-二乙三胺五乙酸二吡哆醇酯(GdDTPA-BPN)和锰-乙二胺四乙酸二吡哆醇酯(MnEDTA-BPN)的弛豫率R₁分别为5.5和3.1L·mmol^-1·s^-1,与其母体螯合物GdDTPA^2-和MnEDTA^2-的R₁值(5.2和2.8L·mmol^-1·s^-1)相当.

Paramagnetic Metal Chelates of DTPA-and EDTA-dipyridoxolester Derivatives and Their NMR T1 Relaxivities in Water

Several novel ligands of DTPAa-nd EDTA-dipyridoxolester derivatives have been synthesized by reaction of DTPA-dianhydride and EDTA-dianhydride with pyridoxol(vitamin B₆) in dry DMF. Their complexes of gadoliniun, manganese and iron were prepared and the measurements of T₁relaxivities in solution of water in vitro were performed with the gadolinium and the manganese complexes. The results show that all of the complexes are highly water soluble and very slightly light and air sensitive both in solid state and in solution. The T₁relaxivities of the complexes, for example, gadolinium-DTPA-dipyridoxolester, GdDTPA-BPN, and manganese-EDTA-dipyridoxolester, MnEDTA-BPN, were determined to be 5.5 and 3.1 L·mmol^-1·s^-1, respectively. These can be compared to the values of the corresponding complexes of their parent ligands, GdDTPA^2-and MnEDTA^2-, indicating the complexes are potentially useful contrast agents for magnetic resonance imaging.