The ketone bodies D-beta-hydroxybutyric acid and acetoacetic acid represent the principal oxidative energy sources of most tissues when dietary glucose is scarce. An ¹⁸F-labeled ketone body could be a useful tool for studying ketone body metabolism using positron emission tomography (PET). Here, we report the first radiofluorinated ketone body derivative (3S)-4-[¹⁸F]fluoro-3-hydroxybutyric acid ([¹⁸F]FBHB) as well as its enantiomer and L-beta-hydroxybutyric acid derivative, (3R)-4-[¹⁸F]fluoro-3-hydroxybutyric acid ((R)-[¹⁸F]F3HB). PET imaging in mice showed biodistribution profiles of the radiotracers that were consistent with the biodistribution of the respective endogenous compounds. Moreover, both enantiomers visualized breast cancer xenografts in vivo. Fasting over 24 h showed significantly enhanced brain and heart uptake of [¹⁸F]FBHB and tumor uptake of (R)-[¹⁸F]F3HB. Disorders exhibiting altered energy substrate utilization, such as Alzheimer's disease, epilepsy, diabetes, and cancer may be of interest for PET imaging studies using [¹⁸F]FBHB.

中文翻译：

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放射性氟化酮体衍生物的合成和体内评价

当膳食葡萄糖稀缺时，酮体D -β-羟基丁酸和乙酰乙酸代表大多数组织的主要氧化能源。18 F 标记的酮体可能是^使用正电子发射断层扫描 (PET) 研究酮体代谢的有用工具。在这里，我们报道了第一个放射性氟化酮体衍生物(3 S )-4-[ ¹⁸ F]氟-3-羟基丁酸([ ¹⁸ F]FBHB)及其对映体和L -β-羟基丁酸衍生物，(3 R )-4-[ ¹⁸ F]氟-3-羟基丁酸(( R )-[ ¹⁸ F]F3HB)。小鼠体内的 PET 成像显示放射性示踪剂的生物分布概况与相应内源性化合物的生物分布一致。此外，两种对映体都使乳腺癌异种移植物在体内可视化。^{禁食超过 24 小时显示大脑和心脏对 [ 18} F]FBHB 的摄取以及肿瘤对 ( R )-[ ¹⁸ F]F3HB的摄取显着增强。^{使用[ 18} F]FBHB的 PET 成像研究可能会对表现出能量底物利用改变的疾病（例如阿尔茨海默病、癫痫、糖尿病和癌症）感兴趣。