一种高稳定性钆类核磁共振成像造影剂的合成.pdf

华东理工大学学报（自然科学版） Journal of East China University of Science and Technology(Natural Science Edition) DOI：10.14135/ki.1006-3080. 20170331003 一种高稳定性钆类核磁共振成像造影剂的合成 程丽坤， 钱伟桥， 丁云， 胡爱国 （华东理工大学材料科学与工程学院，上海市先进聚合物材料重点实验室，上海200237） 摘要：本文合成了一种基于氮氧化二乙烯三胺五乙酸（DTPA ）二异丙胺双酰胺的钆配 1 13 合物，兼具高弛豫率和高稳定性。通过高分辨质谱、核磁谱图（H-NMR 、 C-NMR ）确认 了氮氧化配体及对应的钆配合物的结构，并通过电位滴定法测得其配位稳定性常数。实验结 果表明此配合物的水合常数为3，弛豫率 （16.39 mM-1 ·s-1）达到商用造影剂的3 倍，稳定 性优于商用造影剂Gd-DTPA-BMA （Omniscan® ）且表现出良好的成像效果以及优异的生物 相容性，具有投入临床应用的巨大潜力。 关键词：核磁共振成像造影剂；氮氧化；水合常数；弛豫率；稳定性 中图分类号：O621.3 文献标志码：A Synthesize of a Highly Stable Gadolinium Based MRI Contrast Agent CHENG Li-kun, QIAN Wei-qiao, DING Yun, HU Ai-guo (Shanghai Key Laboratory of Advanced Polymeric Materials, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China) Abstract: Magnetic Resonance Imaging (MRI) is a powerful method for clinical diagnosis and therapy due to the distinguishing characteristics of providing high-quality three-dimensional images of soft tissue without the need for harmful ionizing radiation. Complexes of gadolinium(III) have proven to be especially effective MRI contrast agents, as it is estimated that over 30% of the patients need them to accelerate relaxation rate of in vivo water protons, thus enhancing the contrast of different biological tissues and definition between normal tissues and diseased parts. For more sensitive small-molecule gadolinium-based MRI contrast agents, one essential requirement is to increase the hydration number q, which enhances the gadolinium’s relaxivity. However, with the concern of