• 1964). In vitro metabolism by hepatic microsomal enzymes from rats treated 8 days previously with single i.p. doses of 10 or 100 mg/kg of chlordane in corn oil was increased for the 3 drugs reported (hexobarbital, aminopyrine and chlorpromazine). (inchem.org)
  • the concentration of hexobarbital also plays a role in oxygenase and oxidase activity of hepatic microsomal cytochrome P450. (wikipedia.org)
  • In vivo hexobarbital response, measured by sleeping time of mice, 1, 3 and 8 days after single i.p. doses of 25 mg/kg body-weight technical chlordane or gamma-chlordane, showed a decrease (shortened sleeping time), greatest at day 3 but still marked on day 8 (Fouts, 1963). (inchem.org)
  • Some of the estrogenic contaminants of technical grade methoxychlor are the same as those formed by metabolism in vivo (Bulger et al. (cdc.gov)
  • 1963). Both technical chlordane and one of its pure isomers (gamma-chlordane) have been shown to have stimulating effects on rat liver microsomes for the metabolism of certain drugs (Burns et al. (inchem.org)
  • Hexobarbital or hexobarbitone, sold both in acid and sodium salt forms as Citopan, Evipan, and Tobinal, is a barbiturate derivative having hypnotic and sedative effects. (wikipedia.org)
  • Hexobarbital was long thought to have potentially teratogenic and fetotoxic effects. (wikipedia.org)
  • During World War II, Herta Oberheuser was a Nazi physician and convicted war criminal, investigating the effects of hexobarbital. (wikipedia.org)
  • The biological effects of hexobarbital depend primarily on its ability to penetrate the central nervous system. (wikipedia.org)
  • In Eastern Europe, hexobarbital (and other barbiturates) have been regularly used as drugs by pregnant women attempting suicide. (wikipedia.org)
  • Stoichiometric relationships have been obtained for the hydroxylation of phenylala- nine by hepatic microsomes (26) and the hydroxylation of 17-hydroxy- progesterone by adrenal microsomes (8). (nih.gov)
  • Hexobarbital and the isozyme can form an enzyme-substrate-complex through a hydroxylation reaction, which is involved in the metabolism of xenobiotics. (wikipedia.org)
  • Hepatic metabolism by hydroxylation, oxidation, and glucuronidation. (illumina.com)
  • Trimethylamine has been reported to stimulate NADPH oxidation by an amount equivalent to the amount of trimethylamine oxide formed (2), and hexobarbital was found to increase NADPH oxidation in accordance with stoichiometric expectations (62). (nih.gov)
  • However, in several studies (14, 15, 16, 17) Gillette and coworkers found that some drugs had no effect on NADPH 12-10 oxidation, whereas others had more of an effect than could be accounted for by the metabolism of the drug. (nih.gov)
  • They are substrates for mixed function oxidation and, thus, compete with other xenobiotics for available enzyme, and an intermediate in their metabolism is able to bind with cytochrome P-450 to form an inactive complex which absorbs maximally at 455 nm. (nih.gov)
  • An investigation of the role of microsomal oxidative metabolism in the in vivo genotoxicity of 1,2-dichloroethane. (nih.gov)
  • To evaluate the importance of microsomal oxidative metabolism in the bioactivation of DCE in vivo, male B6C3F1 mice were pretreated with piperonyl butoxide (PIB), an inhibitor of microsomal oxidative metabolism, and the effect of this pretreatment on the extent of hepatic DNA damage produced by DCE was determined 4 hr after DCE administration. (nih.gov)
  • The in vivo genotoxicity of 2-chloroethanol, a product of the microsomal oxidative metabolism of DCE, was also investigated. (nih.gov)
  • Pretreatment of mice with PIB to inhibit microsomal oxidative metabolism significantly potentiated the hepatic DNA damage observed 4 hr after a single, 200-mg/kg, ip dose of DCE. (nih.gov)
  • In addition, they are able to activate xenobiotic metabolism by induction (the increased synthesis and retention) of microsomal oxidative enzymes. (nih.gov)
  • NADPH may serve as an electron donor, via a respiratory chain, direct to cytochrome P-450 with an associated branched pathway to cytochrome bs, the only cytochrome other than cytochrome P-450 found in microsomes. (nih.gov)
  • Scheme showing how NADH and cytochrome bs might contribute to the electron transfer system employed in the microsomal metabolism of drugs SOURCE: Estabrook, R. (11). (nih.gov)
  • One of the cytochrome P450 isozymes is coded by the gene CYP2B1, where hexobarbital is the substrate. (wikipedia.org)
  • the concentration of hexobarbital also plays a role in oxygenase and oxidase activity of hepatic microsomal cytochrome P450. (wikipedia.org)
  • Triacetyl oleandomycin, an inhibitor for isozyme CYP3A4, also inhibits hexobarbital metabolism and biological activity, indicating a close relationship between hexobarbital and cytochrome P450. (wikipedia.org)
  • The inhibition and induction of cytochrome P-450, the central enzyme in the metabolism of xenobiotics, thus provides the focus for consideration of methylenedioxyphenyl synergists as potential hazards. (nih.gov)
  • Another pathway for hexobarbital synthesis is reacting methylcyclohexenylcyanoacetic acid ethyl ester with N-methylurea. (wikipedia.org)
  • Metronidazole may increase the serum concentration of warfarin by decreasing its metabolism. (illumina.com)
  • The first description of the microsomal system: responsible for drug metabolism (39, 40) included a role of nicotinamide-adenine dinucleo- tide reductase (NADH) as well as NADPH. (nih.gov)
  • Moreover, hexobarbital causes the chloride ion channel opening to their longest open state of 9 milli seconds, thereby causing the postsynaptic inhibitory effect to be extended. (wikipedia.org)
  • All in all, hexobarbital causes an CNS-depressant effect on the brain by inhibiting the glutamate release and potentiating the GABA-effect. (wikipedia.org)
  • It has been found over the years that the S(+) enantiomer of hexobarbital potentiates GABAA receptors more effectively than its R(-) enantiomer. (wikipedia.org)