Interaction of chlormezanone enantiomers with rat liver microsomes
| Autor: | E. Karge, Wolfgang Klinger, A. Seeling, H. Oelschläger, D. Rothley |
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| Rok vydání: | 1999 |
| Předmět: |
Male
Chlormezanone law.invention Luminol Lipid peroxidation chemistry.chemical_compound Cytochrome P-450 Enzyme System Coumarins law Oxazines medicine Animals Ethylmorphine Pharmacology (medical) Lucigenin Chromatography High Pressure Liquid Chemiluminescence Pharmacology Chromatography Muscle Relaxants Central Zymosan Anticoagulants Stereoisomerism Hydrogen Peroxide Rats Analgesics Opioid Hexobarbital chemistry Biochemistry Luminescent Measurements Microsomes Liver Acridines Indicators and Reagents Lipid Peroxidation Enantiomer Reactive Oxygen Species Protein Binding medicine.drug |
| Zdroj: | European Journal of Drug Metabolism and Pharmacokinetics. 24:63-68 |
| ISSN: | 2107-0180 0378-7966 |
| DOI: | 10.1007/bf03190012 |
| Popis: | Both chlormezanone enantiomers, for the first time obtained by enantiospecific HPLC with a 100% yield, bind to oxidized cytochrome P-450 in rat liver microsomes with a binding curve according to type I, similar to hexobarbital but less pronounced. There are no differences between the binding curves of the two enantiomers. Ethylmorphine N-demethylation, ethoxycoumarin and ethoxyresorufin O-deethylation are inhibited by both chlormezanone enantiomers at 0.1-1 mM concentrations: no differences could be found. Luminol and lucigenin amplified chemiluminescence indicating the formation of reactive oxygen species was not influenced by either enantiomer in concentration ranges between millimolar and micromolar, whereas hydrogen peroxide formation was inhibited. NADPH/Fe stimulated lipid peroxidation was not influenced. Scavenger activity could not be demonstrated: the zymosan stimulated whole blood chemiluminescence was not influenced significantly. |
| Databáze: | OpenAIRE |
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