Development of C-11-Labeled omega-sulfhydryl fatty acid tracer for myocardial imaging with PET

作者:Wu, Xiangxiang; Wang, Peizhi; Liu, Ruixin; Zeng, Huahui*; Chao, Fangfang; Liu, Hao; Xu, Caiyun; Hou, Haifeng; Yao, Qiong
来源:European Journal of Medicinal Chemistry, 2018, 143: 1657-1666.
DOI:10.1016/j.ejmech.2017.10.062

摘要

[C-11]-S-methyl-16-thiopalmitic acid (a) was developed with excellent heart-to-background uptake ratios and higher retention in heart. Myocardial uptake and metabolism of the tracer is markedly higher CPT I dependent. When compared to [C-11]-S-methyl-14-thiomyristic acid (b), [C-11]-S-methyl-12-thiododecanoic acid (c) and [C-11]-palmitate, a showed an early high uptake and a significantly slower late clearance in heart and a prolonged myocardial elimination half-life (30 min). Analysis of heart tissue and urine samples showed that a was metabolized via beta-oxidation in myocardium. Small animal PET images of the accumulation of a in the rat myocardium were clearly superior to [C-11]-palmitate. These initial studies suggest that a could be a potentially useful clinical PET tracer to assess myocardial fatty acid metabolism.