8-[18F]fluorooctanoic acid and its β-substituted derivatives as potential agents for cerebral fatty acid studies: Synthesis and biodistribution

Fumi Nagatsugi, Shigeki Sasaki, Minoru Maeda

研究成果: ジャーナルへの寄稿学術誌査読

11 被引用数 (Scopus)


Fluorine-18 labeled analogs of 8-fluorooctanoic acid and its structurally modified derivatives with methyl or gem-dimethyl branching or with oxygen substitution at the C3 position were prepared using nucleophilic substitution of the tosylate precursors by [18F]fluoride ion, for evaluation as tracers for cerebral fatty acid metabolism. Tissue distribution studies in rats showed low brain uptakes of these 18F-labeled fatty acid analogs with poor brain-to-blood ratios of activity. The oxygen-substituted analog did not show any significant accumulation of radioactivity in most tissues. The initial brain uptake of activity after injection of ethyl 8-[18F]fluorooctanoate and its free acid remained virtually unchanged over an extended time period. β-Monomethyl and β-gem-dimethyl branched analogs had similar brain uptake at the early time period, but they showed rapid clearance of activity from the brain. TLC analysis showed no incorporation of 8-[18F]fluorooctanoic acid and its β-dimethyl analogs into brain lipids. It was also shown in the metabolite analysis that the labeled metabolites produced from 8-[18F]fluorooctanoic acid are found in blood, and that they could enter the brain to a significant degree. On the contrary, such radioactive metabolites could not be found in the brain in the experiment with the β-gem-dimethyl branched analog. Thus, the present studies showed that retention of radioactivity in the brain with 8-[18F]fluorooctanoic acid derivatives is mainly attributable to their radioactive metabolites, and that the rapid clearance of β-branched analogs from the brain is due to the lack of availability as substrates in the cerebral fatty acid metabolism.

ジャーナルNuclear Medicine and Biology
出版ステータス出版済み - 1月 1 1994

!!!All Science Journal Classification (ASJC) codes

  • 分子医療
  • 放射線学、核医学およびイメージング
  • 癌研究


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