Evaluation of [1-11C]octanoate as a new radiopharmaceutical for assessing liver function using positron emission...

[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.