| 王火强,夏俊勇,赵龙,张志勇,刘兴峰,郑金旭.99mTc-K237的制备及其在小鼠体内分布和显像[J].中国医学影像技术,2009,25(9):1545~1548 |
| 99mTc-K237的制备及其在小鼠体内分布和显像 |
| Preparation of 99mTc-K237 and it’s biodistribution and imaging in mice |
| 投稿时间：2009-03-10 修订日期：2009-04-23 |
| DOI： |
| 中文关键词: 多肽 锝 同位素标记 药代动力学 小鼠 |
| 英文关键词:Peptides Technetium Isotope labeling Pharmacokinetics Mice |
| 基金项目:上海市科学技术委员会科研计划项目(064119647)。 |
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| 中文摘要: |
| 目的 探索99mTc标记多肽K237的方法,研究标记物的稳定性及其在小鼠体内的分布。方法 采用99mTc直接标记多肽K237。正常小鼠尾静脉注射99mTc-K237后不同时间处死,取血液及主要脏器,测定其每克组织百分注射剂量率(%ID/g)。经尾静脉将99mTc-K237注入荷人肺癌A549裸鼠,于注射后不同时间显像。结果 99mTc-K237的标记率和放化纯均＞95%,其与人脐静脉内皮细胞(HUVEC)的最高特异性结合率为40.36%。99mTc-K237在生理盐水和正常人血清中放置24 h后,其放化纯分别为(89.1±1.4)%和(88.3±1.1)% (t=1.56,P＞0.05)。静脉注射99mTc-K237后24 h内,小鼠血液放射性清除迅速,放射性主要聚集在肾脏并经其清除,其他组织器官的放射性随时间逐渐降低。99mTc-K237荷人肺癌A549裸鼠显像示肿瘤组织摄取高,肿瘤与对侧正常组织放射性计数比值(T/NT)最高可达3.97±0.31。结论 99mTc-K237易于制备,具有较理想且符合实际的动物体内动力学表现。 |
| 英文摘要: |
| Objective To explore the method of the radiolabeling of peptide K237 with 99mTc, and to investigate the stability of 99mTc-K237 and it’s distribution and imaging in mice. Methods Peptide K237 was labeled directly with 99mTc. 99mTc-K237 was injected through tail vein of normal mice with 2.96 MBq. Then the mice were killed at different stages after injection and their blood and other major organs were taken out, and the radioactivity counts of these organs were measured to investigate the biodistribution. 99mTc-K237 (5.55 MBq) was injected into the tail vein of tumor bearing nude mice, then imaged at 1, 2, 3, 5 and 8 h. Results Under the best condition, both the labeling rate and the radiochemical purity of 99mTc-K237 were more than 95%. The specific binding efficiency of 99mTc-K237 with human umbilical vein endothelial cell (HUVEC) was 40.36%. After 99mTc-K237 was placed in normal saline and in blood serum, the radiochemical purity was (89.1±1.4)% and (88.3±1.1)% at 24 h, respectively (t=1.56, P＞0.05). In the first 24 h after injection, the biodistribution in mice showed rapid blood and renal clearance with gradually excretion in other organs or tissues, most of the radioactivity was observed in renal. The largest uptake ratio of tumor to non tumor (background) (T/NT) at 3 h was 3.97±0.31. Conclusion 99mTc-K237 can be easily prepared and labeled compound with high labeling rate and stability. |
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