Synthesis and bio‐evaluation of Tc‐99 m‐labeled fatty acid derivatives for myocardial metabolism imaging

Research paper by Jianping Liu, Qianqian Xue, Huan Wang, Hang Wang, Dawei Wang, Yu Fang, Huabei Zhang

Indexed on: 27 Apr '16Published on: 26 Apr '16Published in: Applied Organometallic Chemistry


11C, 18F and 123I fatty acids are used for myocardial imaging, and 99mTc‐labeled fatty acids are more desirable substitutes than other radiolabeled fatty acids. In the work reported, [99mTc]‐CpTT‐10‐oxo‐FPA (), [99mTc]‐CpTT‐12‐oxo‐FPA (), [99mTc]‐CpTT‐14‐oxo‐FPA () and [99mTc]‐CpTT‐16‐oxo‐FPA () were prepared with 60.76–70.92% of radiochemical yield and purity of more than 95%. These radiotracers (, , , ) were chemically stable when incubated in Sprague Dawley rat serum for 3 h at 37 °C. Tissue distribution studies in female mice indicated that had high initial heart uptake (8.84%ID g−1 at 1 min post‐injection) and had long retention in the heart (1.45%ID g−1 at 30 min post‐injection). Metabolite analysis showed could be metabolized to via β‐oxidation with loss of two CH2 in the myocardium, the radiometabolite being excreted via urine. However, low heart uptake suggested that cannot be used as a diagnostic imaging agent. Copyright © 2016 John Wiley & Sons, Ltd.