新型胺羧单酯-酰胺钆配合物的合成及其对大鼠肝区T_1弛豫增强作用

Synthesis and MRI Relaxation Enhancement of Mono-exter-amido Gadolinium Complexes

通过DTPA、EDTA单活化酯与双乳酸酰乙二胺二醇、双乳酸酰己二胺二醇反应,合成了四种新型胺羧单酯鄄酰胺配体及其钆配合物。表征了配体和配合物的结构,测定了钆配合物水溶液水质子的弛豫效能。选取其中一个配合物进行了动物急性毒性测试和活体T1加权成像实验。结果表明:该配合物无明显急性毒性,且对大鼠肝区质子有明显的增强。

Four new ester-amido ligands were synthesized by esterification of mono-iso-butyl diethylenetriaminepen-taacetate and mono-iso-butyl ethylenediaminetetraacetate with N,N'-ethylene bis-lactamide and N,N'-1,6-hexam-ethylenebislactamide,respectively.The corresponding Gd(Ⅲ) complexes were made by reacting the ligands with Gd 2 O 3 .All ligands and complexes were characterized by FT-IR,1 H NMR and elemental analysis.The measured longitudinal relaxivity of these complexes were all higher than that of Gd-DTPA.The investigation on cute toxici-ty and T 1 -weighted imaging of complex derived from mono-N,N'-ethylenebislactamide ester diethlenetriaminepen-taacetate were performed.No cute toxicity was found.The tested complex exhibited the higher enhancement on MRI signal intensity in rat liver,comparing with Gd-DTPA.