European Journal of Medicinal Chemistry p. 1657 - 1666 (2018)
Update date:2022-08-02
Topics:
Wu, Xiangxiang
Wang, Peizhi
Liu, Ruixin
Zeng, Huahui
Chao, Fangfang
Liu, Hao
Xu, Caiyun
Hou, Haifeng
Yao, Qiong
[11C]-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 [11C]-S-methyl-14-thiomyristic acid (b), [11C]-S-methyl-12-thiododecanoic acid (c) and [11C]-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 [11C]-palmitate. These initial studies suggest that a could be a potentially useful clinical PET tracer to assess myocardial fatty acid metabolism.
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