Description and references

Intermediate product of the metabolism of folic acid; the active form into which that acid is converted in the body, ascorbic acid being a necessary factor in the conversion process. First reported as the Leuconostoc citrovorum 8081 growth factor: H. E. Sauberlich, C. A. Baumann, J. Biol. Chem. 176, 165 (1948). Isoln from houseflies: S. Miller, A. S. Perry, Life Sci. 4, 1573 (1965). Prepn: J. A. Brockman, Jr., et al., J. Am. Chem. Soc. 72, 4325 (1950); E. Khalifa et al., Helv. Chim. Acta 63, 2554 (1980). Isomers: D. B. Cosulich et al., J. Am. Chem. Soc. 74, 4215 (1952). Structure: May et al., ibid. 73, 3067 (1951); Pohland et al., ibid. 3247. Manuf: Shive, US 2741608 (1956 to Res. Corp.). Stereoselective synthesis: J. Owens, et al., J. Chem. Soc. Perkin Trans. 1 7, 871 (1993). Used as an antidote to folic acid antagonists such as methotrexate, q.v., which block the conversion of folic acid into folinic acid. Review of clinical combination therapy with methotrexate: J. R. Bertino et al., Ann. N.Y. Acad. Sci. 186, 486-495 (1971). Pharmacokinetics: P. F. Nixon, Clin. Exp. Pharmacol. Physiol. Suppl. 5, 35 (1979). Comprehensive description: L. O. Pont et al., Anal. Profiles Drug Subs. 8, 315-350 (1979). Review of clinical synergy with fluorouracil in cancer: R. J. DeLap, Yale J. Biol. Med. 61, 23-34 (1988).

Properties

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