Abstract Irbesartan was labeled using 125I or 131I with N-bromosuccinimide (NBS) as an oxidizing agent. A lot of operators such as, quantity of substrate, the quantity of oxidizing agent, reaction temperature, reaction time, and pH of reaction medium were studied to optimize high radiochemical yield of [125I]IodoIrbesartan ([125I]Irb.). The preclinical evaluation of IodoIrbesartan in experimental mice indicated high accumulation in target organ of heart with a high heart/blood ratio of 12.85 at 30 min post-injection. This study indicates the suitability of [125I]IodoIrbesartan ([125I]Irb.) for cardiac imaging.

中文翻译：

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厄贝沙坦作为心脏成像示踪剂的放射性碘化和生物学评价

摘要 厄贝沙坦用 125I 或 131I 和 N-溴代琥珀酰亚胺 (NBS) 作为氧化剂进行标记。为了优化[125I]碘厄贝沙坦([125I]Irb.)的高放射化学产率，研究了底物的量、氧化剂的量、反应温度、反应时间和反应介质的pH值等因素。碘厄贝沙坦在实验小鼠中的临床前评估表明，在注射后 30 分钟时，在心脏靶器官中具有高的心血比为 12.85。该研究表明 [125I]IodoIrbesartan ([125I]Irb.) 适用于心脏成像。