Radiosynthesis, rodent biodistribution, and metabolism of 1-deoxy-1-[ 18F]fluoro- d-fructose

• Published in: Nuclear medicine and biology Vol. 22; no. 6; pp. 719 - 725
• Main Authors: Haradahira, Terushi, Tanaka, Akihiro, Maeda, Minoru, Kanazawa, Yoko, Ichiya, Yu-Ichi, Masuda, Kouji
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Inc 01.08.1995; Elsevier
• Subjects: Animals; Biological and medical sciences; Biotransformation; Brain - metabolism; Contrast media. Radiopharmaceuticals; Fibrosarcoma - metabolism; Fluorine Radioisotopes; Fructose - analogs & derivatives; Fructose - chemical synthesis; Fructose - metabolism; Fructose - pharmacokinetics; Indicators and Reagents; Isotope Labeling - methods; Kinetics; Magnetic Resonance Spectroscopy; Male; Medical sciences; Mice; Pharmacology. Drug treatments; Radioisotope Dilution Technique; Rats; Rats, Wistar; Time Factors; Tissue Distribution; In vivo; Radiolabelling; Fluorine; Radioactive tracers; Bioavailability; Metabolism; Pharmacokinetics; Chemical synthesis; Fructose; Radioactivity
• ISSN: 0969-8051; 1872-9614
• DOI: 10.1016/0969-8051(95)00018-S

Fluorine-18 labeled analog of d-fructose, 1-deoxy-1-[ 18F]fluoro- d-fructose (1-[ 18F]FDFrc), was synthesized by nucleophilic substitution of [ 18F]fluoride ion and the effect of the fluorine substitution on its in vivo metabolism was investigated. The tissue distributions of 1-[ 18F]FDFrc in rats and tumor bearing mice showed initial high uptake and subsequent rapid washout of the radioactivity in the principal sites of d-fructose metabolism (kidneys, liver and small intestine). The uptakes in the brain and tumor (fibrosarcoma) were the lowest and moderate, respectively, but tended to increase with time. The in vivo metabolic studies of 1-[ 18F]FDFrc and nonradioactive 1-FDFrc in mouse brain and tumor showed that the fluorinated analog remained unmetabolized in these tissues, indicating that the substitution of fluorine at the C-1 position produces a nonmetabolizable analog of d-fructose. Thus, 1-[ 18F]FDFrc had no features of a metabolic trapping tracer without showing any appreciable organ or tumor specific localization.