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KMID : 1145520180040020057
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Journal of Radiopharmaceuticals and Molecular Probes
2018 Volume.4 No. 2 p.57 ~ p.64
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Synthesis and biodistribution of 18F-labeled α-, β- and ω-fluorohexadecanoic acid
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Lee Yun-Sang
Kim Young-Joo
Cheon Gi-Jeong
Jeong Jae-Min
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Abstract
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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
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KEYWORD
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Myocardial imaging, Positron emission tomography, Radiolabeled fatty acid
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