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目的 研制一种快速、简便、可靠的~99nzTc标记的心血池显像剂.方法 用二氧硫脲(FSA)作人血清白蛋白(HSA)还原剂,用放射性直接标记方法制备~99nzTc标记一步法药盒,测定该药盒及其标记产物的~99nzTc-HSA的理化性质、还原蛋白巯基(-SH)数目及生物性能.结果 对还原后的HSA进行了~99nzTc的标记,放化纯度大于95%,标记后室温放置24小时,放化纯度仍大于95%,体外稳定性很好,小鼠体内分布血中浓度高且较稳定.结论 采用该方法制备的药盒明显提高了~99nzTc-HSA在小鼠体内血中浓度,与~99nzTc-二亚乙基三胺五乙酸一人血清白蛋白(~99nzTc-DTPA-HSA)小鼠体内分布数据二者无显著差异,宜于临床进一步研究.
OBJECTIVE To develop a rapid, simple and reliable ~ 99nzTc-labeled blood pool imaging agent.Methods ~ 99nzTc labeling was performed by radioactive direct labeling with thiourea dioxide (FSA) as a reducing agent for human serum albumin Pharmacokinetics of ~ 99nzTc-HSA in this kit and its labeled product were determined, and the number of thiol groups (-SH) and the biological properties of the reduced protein were determined.Results ~ 99nzTc was labeled in the reduced HSA, and the radiochemical purity was greater than 95%, after labeling for 24 hours at room temperature, radiochemical purity is still greater than 95%, in vitro stability is good, the distribution of blood in mice was high and stable in blood.Conclusion The kit prepared by this method significantly increased ~ 99nzTc- There was no significant difference in the in vivo blood concentration of HSA between the two groups in vivo distribution of ~ 99nzTc-diethylenetriaminepentaacetic acid-human serum albumin (~ 99nzTc-DTPA-HSA) mice, which is suitable for further clinical study.