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19 F nuclear magnetic resonance imaging of drug distribution in vivo: The disposition of an antifolate anticancer drug in mice
Author(s) -
Maxwell R. J.,
Frenkiel T. A.,
Newell D. R.,
Bauer C.,
Griffiths J. R.
Publication year - 1991
Publication title -
magnetic resonance in medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.696
H-Index - 225
eISSN - 1522-2594
pISSN - 0740-3194
DOI - 10.1002/mrm.1910170122
Subject(s) - in vivo , chemistry , pharmacokinetics , magnetic resonance imaging , distribution (mathematics) , drug , ex vivo , pharmacology , nuclear magnetic resonance , in vitro , medicine , biochemistry , biology , radiology , mathematical analysis , physics , microbiology and biotechnology , mathematics
The application of 19 F nuclear magnetic resonance imaging to the study of drug distribution in vivo is discussed. CB3988 (C 2 ‐desamino‐C 2 ‐methyl‐ N 10 ‐propargyl‐2′‐trifluoromethyl‐5,8‐dideazafolic acid) is a fluorinated representative of a class of quinazoline an‐tifolates which act as inhibitors of thymidylate synthase and which are being evaluated for the treatment of human cancer. 19 F images were obtained in vivo from the abdomen of mice following intravenous injection of CB3988 (500 mg/kg). Time resolutions of 4 and 20 min were achieved for two‐ and three‐dimensional imaging, respectively. These images were consistent with the presence of high concentrations of drug (up to 26 mg/ml) in the gall bladder, urinary bladder, and small intestine, as confirmed ex vivo by extraction and HPLC analysis. The results indicate the potential value of 19 F NMR imaging in pharmacokinetic Studies. © 1991 Academic Press, Inc.