Novel 18F-Labeled 1-Hydroxyanthraquinone Derivatives for Necrotic Myocardium Imaging

详细信息    查看全文

• 作者：Ai-Yan Ji ; Qiao-Mei Jin ; Dong-Jian Zhang ; Hua Zhu ; Chang Su ; Xing-Hua Duan ; Li Bian ; Zi-Ping Sun ; Yi-Cheng Ni ; Jian ZhangZhi Yang ; Zhi-Qi Yin
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：February 9, 2017
• 年：2017
• 卷：8
• 期：2
• 页码：191-195
• 全文大小：326K
• ISSN：1948-5875

文摘

Rapid detection and precise evaluation of myocardial viability is necessary to aid in clinical decision making whether to recommend revascularization for patients with myocardial infarction (MI). Three novel ¹⁸F-labeled 1-hydroxyanthraquinone derivatives were synthesized, characterized, and evaluated as potential necrosis avid imaging agents for assessment of myocardial viability. Among these tracers, [¹⁸F]FA3OP emerged as the most promising compound with best stability and highest targetability. Clear PET images of [¹⁸F]FA3OP were obtained in rat model of myocardial infarction and reperfusion at 1 h after injection. In addition, the possible mechanisms of [¹⁸F]FA3OP for necrotic myocardium were discussed. The results showed [¹⁹F]FA3OP may bind DNA to achieve targetability to necrotic myocardium by intercalation. In summary, [¹⁸F]FA3OP was a more promising “hot spot imaging” tracer for rapid visualization of necrotic myocardium.