Covalent binding of a fluorinated 2-nitroimidazole to EMT-6 tumors in Balb/C mice: detection by F-19 nuclear magnetic resonance at 2.35 T.
A hexafluorinated 2-nitroimidazole (CCI-103F) has been synthesized and its properties as a hypoxic cell binder investigated. The drug has a plasma half-life of 90 min in Balb/C mice and a tumor-to-plasma ratio of 0.8. Following sustained exposure to the drug and a washout period for the unbound drug, liver and tumor samples were excised. NMR investigation of the excised tissue in a 2.35 T animal sized NMR facility revealed the presence of 19F bound to both tissues. Further improvement in sensitivity is required to make 19F NMR detection of binding in situ feasible.
D000818:Animals; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008807:Mice, Inbred BALB C; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000378:metabolism*; D009593:Nitroimidazoles / Q000378:metabolism*; D010100:Oxygen / Q000502:physiology; D005466:Fluorocarbons
D009593:Nitroimidazoles; D010100:Oxygen; C049948:CCI 103F; D005466:Fluorocarbons