Metabolism of xilobam in laboratory animals and man
| Autor: | R. S. Egan, W. N. Wu, J. F. Hills |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
Adult
Male medicine.medical_specialty Magnetic Resonance Spectroscopy Adolescent Health Toxicology and Mutagenesis Metabolite Urine Biology Toxicology Biochemistry Mass Spectrometry Excretion chemistry.chemical_compound Mice Dogs Biotransformation Pharmacokinetics Oral administration Internal medicine medicine Animals Humans Rats Wistar Chromatography High Pressure Liquid Pharmacology Mice Inbred ICR Chromatography Muscle Relaxants Central Phenylurea Compounds General Medicine Metabolism Middle Aged In vitro Rats Endocrinology chemistry Liver Female |
| Zdroj: | Xenobiotica; the fate of foreign compounds in biological systems. 24(7) |
| ISSN: | 0049-8254 |
| Popis: | 1. Biotransformation and excretion of xilobam (Xm) were studied after single oral doses of Xm-14C in mouse, rat, dog and man. 2. Following oral administration of Xm-14C, recoveries of total 14C (0-24 h) in urine wereor = 78% of the dose in all species. 3. Xm and a total of 11 metabolites have been isolated and identified, which accounted for 30, 65, 21 and 49% of the total 14C in the urine samples from mouse, rat, dog and man, respectively. 4. Xm was sequentially oxidized at the pyrrolidine ring to form 5'-OH Xm and 5'-oxo Xm. Both metabolites were isolated from human plasma accounting for 61% of the radioactivity in the sample. 5'-OH Xm was also identified as a major in vitro metabolite in the 9000g supernatant from a rat liver homogenate preparation. 5. 5'-OH Xm was isolated from the urine of all species except rats. However, oxidation products of 5'-oxo Xm were also present. Oxidation at the phenyl (ph) ring and at the phCH3 group produced the corresponding 4-OHph and phCH2OH metabolites. Subsequent water addition at the 2-position of the pyrrolidine ring followed by cleavage and/or cyclization of the above metabolites resulted in six additional urinary metabolites. |
| Databáze: | OpenAIRE |
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