基于双功能螯合剂的99mTc间接标记depreotide的探索

Indirect labeling of depreotide with 99mTc using bifunctional chelating agents

关键词:  双功能螯合剂  depreotide  间接标记  小鼠

Key words:  double function chelating agent  depreotide  indirect mark  mouse

摘要:

目的 探索使用采用双功能螯合剂作为偶联剂进行间接标记,以避免直接标记所带来的损伤。方法 使用近年来常用的三种螯合剂HYNIC、NHS-MAG3及SHNH进行间接标记。结论 三种标记体系的标记率、放化纯及比活度较高,为核素分子显像提供了必要的基础条件和临床应用前景。稳定性测定发现^99mTc-MAG3-depreotide在室温、血清以及血浆中更稳定。^99mTc HYNIC-depreotide和^99mTc-SHNH-depreotide在血液、心脏、胃、肠的分布显著较高。而^99mTc-MAG3-depreotide标记物主要经过肾脏排出体外,在血液、肝脏和肾脏中清除较快,而心脏、肺、肌肉、骨骼和脑组织放射性分布均较低,且在整个过程中变化不显著。

Abstract:

Objective To explore the use of bifunctional chelating agents for indirect ^99mTc-labeling of depreotide.Methods Three kinds of chelating agents HYNIC,NHS-MAG3 and SHNH were applied for indirect labeling of depreotide with ^99mTc.Results All three labeling systems had high labeling rate,radiochemistry purity and activity.^99mTc-MAG3-depreotide was more stable in room temperature,serum and plasma.The distribution of ^99mTc-HYNIC-depreotide and ^99mTc-SHNHdepreotide was significantly higher in blood,heart,stomach and intestine.^99mTc-MAG3-depreotide was mainly excreted from kidney;its clearance in the blood,liver and the kidney was faster,and the radioactive distribution in heart,lung,muscle,bone and brain tissue was lower.Conclusion Indirect ^99mTc-labeling of depreotide using bifunctional chelating agents may provide necessary laboratory basis for its future clinical application.