Bunolol metabolism by cell-free preparations of human liver: biosynthesis of dihydrobunolol
| Autor: | Harvey R. Kaplan, R. Clive Greenough, Charles F. Schwender, Frederick J. Di Carlo, Franz Josef Leinweber |
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| Rok vydání: | 1972 |
| Předmět: |
Adult
Male Magnetic Resonance Spectroscopy Infrared Rays Ultraviolet Rays Health Toxicology and Mutagenesis Metabolite Reductase Biology Pharmacology Toxicology Biochemistry Cell-free system chemistry.chemical_compound Biosynthesis Humans Aged chemistry.chemical_classification Human liver Cell-Free System Spectrum Analysis Hemodynamics Isoproterenol General Medicine Metabolism Middle Aged Amino Alcohols Cytosol Alcohol Oxidoreductases Kinetics Enzyme chemistry Liver Levobunolol Sympatholytics Female Chromatography Thin Layer Hydrogenation |
| Zdroj: | Xenobiotica; the fate of foreign compounds in biological systems. 2(2) |
| ISSN: | 0049-8254 |
| Popis: | 1. Cell-free preparations from human liver taken at autopsy were used to biosynthesize a metabolite from bunolol. The metabolite was isolated and identified as dihydrobunolol on the basis of elemental analysis, n.m.r., i.r. and u.v. spectrometry, and inability to form a 2,4-dinitrophenylhydrazone.2. The identification was confirmed by the subsequent synthesis of dihydrobunolol and comparative studies including t.l.c., n.m.r., i.r. and u.v. spectrometry.3. The livers of ten cadavers contained the reductase which was located in the cytosol. The enzyme utilized NADPH more effectively than NADH. At a higher pH, the same liver fraction extensively converted dihydrobunolol to bunolol.4. Synthetic dihydrobunolol was as active as bunolol in antagonizing isoproterenol-induced changes in blood pressure, heart rate and contractile force after intravenous administration to the dog. |
| Databáze: | OpenAIRE |
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