9978. Vigabatrin

Description and references

Irreversible inhibitor of γ-aminobutyric acid transaminase, the enzyme responsible for the degradation of the neurotransmitter γ-aminobutyric acid (GABA). Prepn: B. W. Metcalf, M. Jung, US 3960927 (1976 to Richardson-Merrell); and in vitro enzyme inactivation: B. Lippert et al., Eur. J. Biochem. 74, 441 (1977). Mechanism of action study: P. J. Schechter et al., Eur. J. Pharmacol. 45, 319 (1977). Anticonvulsant activity and toxicity studies: W. Lscher, Neuropharmacology 21, 803 (1982). HPLC determn in plasma and urine: J. A. Smithers et al., J. Chromatogr. 341, 232 (1985). The S(+)-enantiomer is the pharmacologically active form. Pharmacokinetics of enantiomers in humans: K. D. Haegele, P. J. Schechter, Clin. Pharmacol. Ther. 40, 581 (1986). Clinical studies in treatment resistant epilepsy: C. A. Tassinari et al., Arch. Neurol. 44, 907 (1987); T. R. Browne et al., Neurology 37, 184 (1987). Series of articles on clinical use in adult and childhood epilepsy: J. Child Neurol. 6, Suppl. 2, S3-S69 (1991). Reviews of early literature and mechanism of action: M. J. Iadarola, K. Gale, Mol. Cell. Biochem. 39, 305-330 (1981); of pharmacology and toxicology: E. J. Hammond, B. J. Wilder, Clin. Neuropharmacol. 8, 1-12 (1985). Review: S. M. Grant, R. C. Heel, Drugs 41, 889-926 (1991).

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