Metabolism of detomidine in the rat II. Characterisation of metabolites in urine
| Autor: | Maire Eloranta, Jarmo S. Salonen, Lauri Vuorilehto, Karjalainen Arto Johannes |
|---|---|
| Rok vydání: | 1988 |
| Předmět: |
Male
Agonist Magnetic Resonance Spectroscopy Silylation medicine.drug_class Metabolite Urine Mass Spectrometry chemistry.chemical_compound Biotransformation medicine Animals Hypnotics and Sedatives Pharmacology (medical) Solid phase extraction Chromatography High Pressure Liquid Pharmacology Detomidine Chromatography Imidazoles Rats Inbred Strains Metabolism Reference Standards Rats chemistry Biochemistry Chromatography Thin Layer medicine.drug |
| Zdroj: | European Journal of Drug Metabolism and Pharmacokinetics. 13:59-65 |
| ISSN: | 2107-0180 0378-7966 |
| Popis: | In order to investigate the biotransformation of a new alpha 2-adrenoceptor agonist, detomidine, metabolites were isolated from rat urine by solid phase extraction and purified by TLC. The isolated compounds were structurally analysed by 1H-NMR, MS and GC-MS as such or as their methyl and/or silyl derivatives. In addition to detomidine, which was found in trace amounts, four major metabolites were identified: hydroxymethyldetomidine, the corresponding O-glucuronide, detomidine carboxylic acid, and detomidine mercapturate. Together the identified components make up about 80% of urinary detomidine derived compounds. On the basis of these findings a major biotransformation pathway could be suggested. The reaction sequence is initiated by a hydroxylation. Subsequent glucuronidation, glutathione conjugation or secondary oxidation divide the route into three branches each producing one of the other three identified metabolites. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink