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Development of 11C-Labeled ω-sulfhydryl fatty acid tracer for myocardial imaging with PET
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2017-10-23 , DOI: 10.1016/j.ejmech.2017.10.062
Xiangxiang Wu , Peizhi Wang , Ruixin Liu , Huahui Zeng , Fangfang Chao , Hao Liu , Caiyun Xu , Haifeng Hou , Qiong Yao

[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.



中文翻译:

用于PET心肌成像的11 C标签ω-巯基脂肪酸示踪剂的开发

[ 11 C] -S-甲基-16-硫代棕榈酸(a)具有优异的心脏与背景摄取比和更高的心脏保留率。示踪剂的心肌摄取和代谢明显取决于CPTI。当与[ 11 C] -S-甲基-14-硫代肉豆蔻酸(b),[ 11 C] -S-甲基-12-硫代十二酸(c)和[ 11 C] -棕榈酸相比时,a表现出较高的早期摄取并显着减慢了心脏的后期清除速度,延长了心肌消除半衰期(30分钟)。心脏组织和尿液样本的分析表明,在心肌中通过β-氧化代谢。大鼠心肌中a积累的小动物PET图像明显优于[ 11 C]棕榈酸酯。这些初步研究表明,a可能是评估心肌脂肪酸代谢的潜在有用的临床PET示踪剂。

更新日期:2017-10-23
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