Synthesis and biodistribution of 18F-labeled α-, β- and ω-fluorohexadecanoic acid
이윤상, 김영주, 천기정, 정재민,
소속 상세정보
이윤상 ( Lee Yun-Sang )
Seoul National University College of Medicine Department of Nuclear Medicine
김영주 ( Kim Young-Joo )
Seoul National University College of Medicine Department of Nuclear Medicine
천기정 ( Cheon Gi-Jeong )
Seoul National University College of Medicine Department of Nuclear Medicine
정재민 ( Jeong Jae-Min )
Seoul National University College of Medicine Department of Nuclear Medicine
Abstract
ω-[18F]-Fluorohexadecanoic acid (FHA) has been used for imaging of fatty acid metabolism of myocardium. To increase retention of radiolabeled fatty acid by blocking β-oxidation, methyl branched analogues have been used. In this experiment, we tried to synthesize 18F-labeled α-, β- and ω-FHA for imaging of the myocardial fatty acid metabolism. We synthesized α-, β- and ω-mesylated methyl hexadecanoates and labeled with 18F by reacting with [18F]TBAF in acetonitrile at 80ºC for 10 min. Methyl ester group was removed by 1 M NaOH at 80ºC for 5 min. The yields of α-[18F] and ω-[18F]FHA were 25.5 and 45.5%, respectively [EOS]. However, β-[18F] FHA was not labeled at all due to a fast elimination reaction. The biodistribution study in ICR-mice showed that ω-[18F]FHA has higher myocardial uptake and lower liver uptake than α-[18F]FHA. The electron-withdrawing effect of fluorine at α- position is believed to be the major factor affecting the biodistribution
키워드
Myocardial imaging; Positron emission tomography; Radiolabeled fatty acid
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