Human moricizine metabolism. I. Isolation and identification of metabolites in human urine
| Autor: | H. J. Pieniaszek, J. M. Read, P. N. Confalone, G. O. Page, A. F. Davidson, L. E. Richards, S. Shatzmiller, K. F. Blom |
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| Rok vydání: | 1997 |
| Předmět: |
Adult
Male Carbamate Stereochemistry Health Toxicology and Mutagenesis medicine.medical_treatment Metabolite Urine Toxicology Biochemistry chemistry.chemical_compound Oral administration Phenothiazine medicine Moracizine Humans Prodrugs Pharmacology Moricizine Molecular Structure General Medicine Metabolism chemistry Female Anti-Arrhythmia Agents medicine.drug |
| Zdroj: | Xenobiotica; the fate of foreign compounds in biological systems. 27(2) |
| ISSN: | 0049-8254 |
| Popis: | 1. Using synthetic standards and/or spectral data, seven moricizine metabolites were structurally identified in human urine. Two novel metabolites were identified as phenothiazine-2-carbamic acid and ethyl [10-(3-aminopropionyl) phenothiazin-2-yl] carbamate. Two novel human moricizine metabolites, 2-amino-10-(3-morpholino-propionyl) phenothiazine, a previously identified dog metabolite, and 2-aminophenothiazine, a previously identified rat metabolite, were also identified. Three additional human metabolites, phenothiazine-2-carbamic acid ethyl ester sulphoxide (P2CAEES), moricizine sulphoxide, and ethyl ?10-[N-(2'-hydroxyethyl)3-aminopropionyl] phenothiazin-2-yl? carbamate, all previously described in the literature, were observed. 2. Both 2-amino-10-(3-morpholinopropionyl) phenothiazine and ethyl [10-(3-aminopropionyl) phenothiazin-2-yl] carbamate, and possibly ethyl ?10-[N-(2'-hydroxyethyl) 3-aminopropionyl]phenothiazin-2-yl? carbamate, possess the structural characteristics thought to be necessary for class 1 antiarrhythmic activity. |
| Databáze: | OpenAIRE |
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