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

作者：Ji, Ai-Yan; Jin, Qiao-Mei; Zhang, Dong-Jian; Zhu, Hua; Su, Chang; Duan, Xing-Hua; Bian, Li; Sun, Zi-Ping; Ni, Yi-Cheng; Zhang, Jian^*; Yang, Zhi^*; Yin, Zhi-Qi^*

来源：ACS Medicinal Chemistry Letters, 2017, 8(2): 191-195.

DOI：10.1021/acsmedchemlett.6b00398

• Myocardial infarction
• necrosis avid agents
• anthraquinone
• F-18
• positron emission tomography

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 F-18-labeled 1-hydroxyanthraquinone derivatives were synthesized, characterized, and evaluated as potential necrosis avid imaging agents for assessment of myocardial viability. Among these tracers, [F-18]FA3OP emerged as the most promising compound with best stability and highest targetability. Clear PET images of [F-18]FA3OP were obtained in rat model of myocardial infarction and reperfusion at 1 h after injection. In addition, the possible mechanisms of [F-18]FA3OP for necrotic myocardium were discussed. The results showed [F-19]FA3OP may bind DNA to achieve targetability to necrotic myocardium by intercalation. In summary, [F-18]FA3OP was a more promising "hot spot imaging" tracer for rapid visualization of necrotic myocardium.

• 出版日期2017-2
• 单位江苏省中医药研究院; 南京中医药大学; 山东省医学科学院; 中国药科大学; 北京大学