Positron labeled antioxidants: synthesis and tissue biodistribution of 6-deoxy-6-[18F]fluoro-L-ascorbic acid.
A one-pot synthesis of 6-deoxy-6-[18F]fluoro-L-ascorbic acid (18F-DFA) has been developed via nucleophilic displacement of a cyclic sulfate with no-carrier-added [18F]fluoride ion. Isolated radiochemical yields of around 15% were obtained with radiochemical purity of over 99% after overall synthesis time of 90 min. Tissue distribution studies with 18F-DFA in rats showed high uptake of radioactivity in the adrenals, kidneys, liver and small intestine--organs known to have high concentrations of L-ascorbic acid. The slow and low uptake of radioactivity in the brain was observed between 10 and 120 min after i.v. injection. In vivo behavior of 18F-DFA in mice bearing 3-methylcholanthrene-induced fibrosarcoma demonstrated its ability to accumulate in the tumor.
Yamamoto
F
F
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Sasaki
S
S
Maeda
M
M
D000818:Animals; D000975:Antioxidants / Q000493:pharmacokinetics*; D001205:Ascorbic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D005462:Fluorine Radioisotopes; D007553:Isotope Labeling; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D000975:Antioxidants; D005462:Fluorine Radioisotopes; C076401:6-deoxy-6-fluoroascorbic acid; D001205:Ascorbic Acid