核化学与放射化学2012，Vol.34Issue(1)：27-33,7.
不同电荷肿瘤乏氧显像剂的合成及生物分布
Preparation and Biodistribution of Tumor Hypoxia Imaging Agents With Different Charges
摘要
Abstract
The charge is an important characteristic of a drug molecule. The overall charge on a drug affects its pharmacological properties in vivo. In this study, (S)-methyl 3-(4-hydroxyphenyl)-2-(3-(2-nitro-lH-imidazol-l-yl)propanamido)propanoate (NI-Y-M), (S)-3-(4-hydroxyphenyl)-2-(3-(2-nitro-lH-imidazol-l-yl)propanamido) propanoic acid (NI-Y) and (S)-N-(3-aminopropyl)-3-(4-hydroxyphenyl)-2-(3-(2-nitro-lH-imidazol-l-yl) propanamido) propanamide (NI-Y-A) were synthesized and radioiodinated with 131I. All the radioiodinated compounds are obtained in >95% yield determined by HPLC and stable at room temperature for 24 h in vitro. The paper electrophoresis results indicate that the compounds formed are different in charge, [131]NI-Y-M, [131I]NI-Y, and [131]NI-Y-A are neutral, negative andpositive, respectively. The biodistribution results in mice bearing S180 tumor demonstrate that all of the [131]NI-Y-M, [131] NI-Y and [131] NI-Y-A accumulate in tumor fast and slowly clear from it. The uptakes in tumor are higher than those in muscle, heart, brain and spleen. The tumor-to-tissue ratios increase along with time. At 4 h post injection, the uptake ratios of tumor-to-muscle and tumor-to-blood indicate that among them the positively charged [131] NI-Y-A is the best hypoxia agent.关键词
乏氧显像剂/2-硝基咪唑/131I标记/电荷/生物分布Key words
hypoxia imaging agent/2-nitroimidazole/131I radioiodination/charge/biodistribution分类
医药卫生引用本文复制引用
黄士堂,王祥云,褚泰伟..不同电荷肿瘤乏氧显像剂的合成及生物分布[J].核化学与放射化学,2012,34(1):27-33,7.基金项目
国家自然科学基金资助项目(20771011,21071010,91026011) （20771011,21071010,91026011）
