JOURNAL ARTICLE

Synthesis and in vivo evaluation of a radiofluorinated ketone body derivative

Stephanie J Mattingly, Melinda Wuest, Eugene J Fine, Ralf Schirrmacher, Frank Wuest
RSC medicinal chemistry 2020 February 1, 11 (2): 297-306
33479637
The ketone bodies d-beta-hydroxybutyric acid and acetoacetic acid represent the principal oxidative energy sources of most tissues when dietary glucose is scarce. An 18 F-labeled ketone body could be a useful tool for studying ketone body metabolism using positron emission tomography (PET). Here, we report the first radiofluorinated ketone body derivative (3 S )-4-[18 F]fluoro-3-hydroxybutyric acid ([18 F]FBHB) as well as its enantiomer and l-beta-hydroxybutyric acid derivative, (3 R )-4-[18 F]fluoro-3-hydroxybutyric acid (( R )-[18 F]F3HB). PET imaging in mice showed biodistribution profiles of the radiotracers that were consistent with the biodistribution of the respective endogenous compounds. Moreover, both enantiomers visualized breast cancer xenografts in vivo . Fasting over 24 h showed significantly enhanced brain and heart uptake of [18 F]FBHB and tumor uptake of ( R )-[18 F]F3HB. Disorders exhibiting altered energy substrate utilization, such as Alzheimer's disease, epilepsy, diabetes, and cancer may be of interest for PET imaging studies using [18 F]FBHB.

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