摘要/Abstract

磁共振成像技术被广泛应用于诊断医学和软组织成像，而磁共振对比剂有助于提高成像对比度.报道了两种基于钆-DOTA-酰肼结构的新型双核非离子型磁共振对比剂[（Gd-DOTAH）₂-DYMB和（Gd-DOTAH）₂-DYMBP]的设计、合成及弛豫性能.在0.5 T磁场下，测得其纵向弛豫率分别为每分子11.4和11.7 L·mmol^-1·s^-1或5.7和5.9 L·mmol^-1· Gd^-1·s^-1，高于目前临床使用的单核大环对比剂钆-DOTA.体外磁共振成像研究显示该两种磁共振对比剂具有提高诊断灵敏度和准确度的应用潜力.
关键词: 磁共振成像, 对比剂, 合成, 弛豫率, DOTA-酰肼, 钆-DOTA
Magnetic resonance imaging (MRI) is widely used in diagnostic medicine and soft tissue imaging. Contrast agents (CAs) can improve the specificity of MRI enhancement. Herein, the design, synthesis and relaxivity of two novel binuclear nonionic Gd-based DOTA-hydrazide derived MRI contrast agents, (Gd-DOTAH)₂-DYMB and (Gd-DOTAH)₂-DYMBP are reported. They have improved longitudinal relaxivity values of 11.4 and 11.7 L·mmol^-1·s^-1 per molecule or 5.7 and 5.9 L·mmol^-1·Gd^-1·s^-1 at 0.5 T, respectively, which are higher than that of the mononuclear clinical macrocyclic agent Gd-DOTA. And in vitro MRI studies suggest the potential of these two agents as MRI contrast agents in improving the diagnostic sensitivity and accuracy.
Key words: magnetic resonance imaging (MRI), contrast agents, synthesis, relaxivity, DOTA-hydrazide, Gd-DOTA


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