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
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.

Full Text Links

Find Full Text Links for this Article


You are not logged in. Sign Up or Log In to join the discussion.

Trending Papers

Remove bar
Read by QxMD icon Read

Save your favorite articles in one place with a free QxMD account.


Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"