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

ACS Med Chem Lett

Department of Natural Medicinal Chemistry & Jiangsu Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, Jiangsu, China.

Published: February 2017

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

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5304286PMC
http://dx.doi.org/10.1021/acsmedchemlett.6b00398DOI Listing

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