Abstract

Azilsartan (AZ) was labeled with ¹³¹I using Chloramine-T as oxidizing agent. Factors affecting the labeling efficiency were systematically studied, and optimum conditions were found: oxidizing agent amount 100 μg, substrate amount 100 μg, pH 6, reaction time 30 min, and ambient temperature. Biodistribution studies showed that [¹³¹I]iodoAZ is concentrated in heart at 5 min post-injection to give high uptake of 29.0 ± 0.6% injected dose/g organ. Thus, iodoAZ shows promise as a radiotracer for heart imaging.

中文翻译：

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放射性碘化阿齐沙坦作为一种用于心肌灌注成像的新型高选择性放射性示踪剂

摘要

Azilsartan (AZ) 用¹³¹ I标记，使用 Chloramine-T 作为氧化剂。系统研究了影响标记效率的因素，确定了最佳条件：氧化剂用量100 μg，底物用量100 μg，pH 6，反应时间30 min，环境温度。生物分布研究表明，[ ¹³¹ I]iodoAZ 在注射后 5 分钟时集中在心脏中，以提供 29.0 ± 0.6% 注射剂量/g 器官的高摄取。因此，iodoAZ 显示出作为心脏成像放射性示踪剂的前景。