^<18>F-Labeled Octanoates as Potential Agents for Cerebral Fatty Acid Studies. The Influence of 4-Substitution and the Fluorine Position on Biodistribution
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概要
- 論文の詳細を見る
In order to understand the structural features that might lead to an in vivo radiotracer for studying cerebral fatty acid metabolism, 8-[^<18>F]fluorooctanoate derivatives with methyl or gem-dimethyl branching at the C4 position have been prepared. 3-[^<18>F]Fluoro- and 4-[^<18>F]fluorooctanoic acid have also been synthesized for studying the influence of the fluorine position on the in vivo behavior of ^<18>F-labeled octanoic acid analogs. Radiochemical synthesis was achieved by the nucleophilic displacement of a tosylate or mesylate precursor with [^<18>F]fluoride ion. Tissue distribution studies in rats showed low cerebral uptakes of these ^<18>F-labeled fatty acid analogs with poor brain-to-blood ratios. 3-[^<18>F]Fluorooctanoic acid showed considerable defluorination, evident as a high bone activity level. The initial uptake of activity in the brain after injection of ethyl 8-[^<18>F]fluoro-4-methyloctanoate and 4-[^<18>F]-fluorooctanoic acid remained virtually unchanged over an extended time period, similar to that previously observed for the unbranched analogs, ethyl 8-[^<18>F]fluorooctanoate and its free acid. In contrast, the 4-gem-dimethyl branched analog was rapidly and preferentially taken up by the liver. It was shown in the metabolite analysis that labeled metabolites produced from 8-[^<18>F]fluoro-4-methyloctanoic acid were found in blood, and that the they could enter the brain to a significant degree. Thus, the present studies showed that radioactivity retention in the brain in the case of the 4-methyl branched analog was mainly attributable to its radioactive metabolites.
- 社団法人日本薬学会の論文
- 1995-04-15
著者
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前田 稔
九州大学大学院薬学研究院
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前田 稔
Faculty of Pharmaceutical Sciences, Kyusyu University
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佐々木 茂貴
Faculty of Pharmaceutical Sciences, Kyusyu University
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井上 富美子
Faculty Of Pharmaceutical Sciences Kyushu University
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前田 稔
九州大学薬学部放射性薬品化学
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Inoue Fumiko
Faculty Of Pharmaceutical Sciences Kyushu University
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佐々木 茂貴
九州大学薬学部放射性薬品化学
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永次 史
Faculty of Pharmaceutical Sciences, Josai University
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佐々木 茂貴
Faculty Of Pharmaceutical Sciences Kyushu University
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永次 史
九州大学大学院薬学研究院
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Nagatsugi Fumi
Faculty Of Pharmaceutical Sciences Kyushu University
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永次 史
Faculty Of Pharmaceutical Sciences Josai University
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Inoue F
Faculty Of Pharmaceutical Sciences Kyushu University
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前田 稔
Faculty Of Pharmaceutical Sciences Kyushu University
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