TY - JOUR
T1 - Positron labeled antioxidants
T2 - Synthesis and tissue biodistribution of 6-deoxy-6-[18F]fluoro-l-ascorbic acid
AU - Yamamoto, Fumihiko
AU - Sasaki, Shigeki
AU - Maeda, Minoru
N1 - Funding Information:
Acknowledgements-The support of this work by a Grant-m-Aid for Sclentdic Research from the Mmlstry of Education, Science and Culture of Japan, and by a grant from the Ministry of Health and Welfare of Japan are gratefully acknowledged We are Indebted to the staff of the Kyushu University Medical School Cyclotron Faclhty for their assistance m producing 18F
PY - 1992/5
Y1 - 1992/5
N2 - 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.
AB - 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.
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U2 - 10.1016/0883-2889(92)90032-A
DO - 10.1016/0883-2889(92)90032-A
M3 - Article
C2 - 1325422
AN - SCOPUS:0026572534
SN - 0969-8043
VL - 43
SP - 633
EP - 639
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
IS - 5
ER -