硝基咪唑类在肿瘤乏氧显像剂中的作用和研究进展  

Progress in study of nitroimidazole as hypoxia imaging agents in tumor

作　　者：杨怡君[1] 丁劲松[1] 

机构地区：[1]中南大学药学院,湖南长沙410013

出　　处：《药学学报》2016年第8期1227-1232,共6页Acta Pharmaceutica Sinica

摘　　要：放射性核素乏氧显像已成为肿瘤诊断、治疗中的重要手段。有相当数量的硝基咪唑类化合物作为乏氧显像剂用于临床前及临床研究。如何设计出理想的显像剂结构正逐步成为新型显像剂开发的关键。显像剂中硝基咪唑的类型和数量、连接基团的结构和化合物手性等都直接影响显像效果;而显像剂整体的性质如单电子还原电势、油水分配系数及药物动力学特征也是关键因素。本文通过探讨影响硝基咪唑类化合物显像效果的因素,为显像剂的设计提供一定的思路。Radionuclide hypoxia imaging has become an indispensable core of tumor diagnosis. Nitroimidazole derivatives have been extensively used as the hypoxia imaging agents in preclinical and clinical research. It is the key to design the ideal structure for promising agents. The type and quantity of nitroimidazole, the linker structure and chiral may have an impact on the imaging results. The characteristics of the imaging agents including single electron reduction potential（SERP）, oil-water partition coefficient（log P） and pharmacokinetics are also the key factors. In this review, we highlight the factors for hypoxia imaging, providing clues for the structure design of new agents.

关 键 词：放射性核素 肿瘤显像剂 乏氧 硝基咪唑 肿瘤靶向 结构设计 诊断治疗 

分 类 号：R916[医药卫生—药学]