Yamamura N, Magata Y, Kitano H, Konishi J, Saji H
Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Japan.
Nucl Med Biol. 1998 Jul;25(5):467-72. doi: 10.1016/s0969-8051(98)00011-0.
[1-11C]Octanoate was evaluated as a new radiopharmaceutical for the evaluation of liver function using positron emission tomography (PET). In biodistribution studies with normal mice, [1-11C]octanoate was rapidly taken up by the liver. [1-11C]Octanoate in the liver was present in the parenchymal cells and was predominantly metabolized via beta-oxidation followed by its rapid clearance. In the CCl4-treated mice, [1-11C]octanoate showed significantly slower hepatic clearance than that in the controls. In PET studies using rats, the time-radioactivity curves in the liver showed a two-phase decrease, and compared with the normal rat, the CCl4-treated rat showed a slower hepatic half-clearance time for the first phase, which is related to beta-oxidation metabolism. A preliminary PET study of [1-11C]octanoate metabolism in a normal volunteer was consistent with these animal studies. The present study showed that metabolism of [1-11C]octanoate in the liver was influenced by beta-oxidation, and it is advantageous to use [1-11C]octanoate clinically as a regional liver-function diagnostic agent in conjunction with PET.
[1-¹¹C]辛酸酯作为一种新型放射性药物，通过正电子发射断层扫描（PET）用于评估肝功能。在对正常小鼠的生物分布研究中，[1-¹¹C]辛酸酯被肝脏迅速摄取。肝脏中的[1-¹¹C]辛酸酯存在于实质细胞中，主要通过β-氧化代谢，随后迅速清除。在四氯化碳处理的小鼠中，[1-¹¹C]辛酸酯的肝脏清除速度明显慢于对照组。在对大鼠的PET研究中，肝脏中的时间-放射性曲线呈两相下降，与正常大鼠相比，四氯化碳处理的大鼠在第一阶段的肝脏半清除时间较慢，这与β-氧化代谢有关。对一名正常志愿者进行的[1-¹¹C]辛酸酯代谢的初步PET研究与这些动物研究结果一致。本研究表明，肝脏中[1-¹¹C]辛酸酯的代谢受β-氧化影响，临床上将[1-¹¹C]辛酸酯与PET结合用作区域性肝功能诊断剂具有优势。
