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Stiripentol is an anti-epileptic drug of novel structure with previously demonstrated strong in vitro inhibitory activity on rat cerebral cytochrome P-450 mediated naphthalene hydroxylation [6]. When administered to rats as a single i.p. dose, the drug is presently shown to have the same in vitro effect. Maximal inhibition is seen 2 hr after administration, but at this time the brain concentrations of intact drug, although peaking, appear too low (ca. 11 micrograms/g tissue) to account for the intensity of the effect seen in vitro. This suggests in vivo activation to a metabolic intermediate forming a complex with cerebral cytochrome P-450, which 2 hr after dosing is fully insensitive to stiripentol added to incubates. Restoration of enzymic activity and of sensitivity to added stiripentol occurs progressively and is practically complete 24 hr after dosing.
M Mesnil, and
B Testa, and
P Jenner
January 1991,
Epilepsia,
M Mesnil, and
B Testa, and
P Jenner
March 1982,
Molecular pharmacology,
M Mesnil, and
B Testa, and
P Jenner
January 1979,
Drug and chemical toxicology,
M Mesnil, and
B Testa, and
P Jenner
March 1987,
Neuroscience,
M Mesnil, and
B Testa, and
P Jenner
July 1985,
Archives of biochemistry and biophysics,
M Mesnil, and
B Testa, and
P Jenner
November 1986,
Science (New York, N.Y.),
M Mesnil, and
B Testa, and
P Jenner
January 1988,
Biochemical and biophysical research communications,
M Mesnil, and
B Testa, and
P Jenner
December 1992,
The Biochemical journal,
M Mesnil, and
B Testa, and
P Jenner
May 1984,
Xenobiotica; the fate of foreign compounds in biological systems,
M Mesnil, and
B Testa, and
P Jenner
January 1996,
Nutrition and cancer,
