氮杂大环化合物可作为双功能螯合剂标记生物分子(一般为小肽,蛋白质或单克隆抗体等),这些放射性金属标记的生物分子为核医学提供了具有广阔应用前景的放射性诊断和放射性治疗药物。综述了氮杂大环化合物在放射性金属标记中的应用研究最新进展,介绍了用于标记的氮杂大环化合物,用于标记的放射性核素,以及标记物的生物学特性。并指出了氮杂大环化合物在不同核素标记中的优缺点。 Aza macrocycles can be used as bi-functional chelators to label biomolecules (usually small peptides, proteins or monoclonal antibodies, etc.). These biomolecules labeled with radioactive metals provide nuclear medicine a broad spectrum of applications in radiodiagnosis and radiotherapy drug. The recent progress in the application of aza-macrocycles in radioactive metal labeling is reviewed. The aza-macrocycles for labeling, the radionuclides for labeling, and the biological characteristics of the labels are introduced. The advantages and disadvantages of aza-macrocycles in different nuclide labeling are pointed out.