Metabolic chiral inversion of ibuprofen in isolated rat hepatocytes
Autor: | Sylvia Müller, Joachim M. Mayer, Bernard Testa, Jean-Claude Etter |
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Rok vydání: | 1990 |
Předmět: |
Pharmacology
Liver cytology Stereochemistry Chemistry organic chemicals Organic Chemistry Kinetics Stereoisomerism Ibuprofen Inversion (discrete mathematics) Catalysis Analytical Chemistry In vitro model medicine.anatomical_structure Liver metabolism Hepatocyte Drug Discovery medicine Spectroscopy medicine.drug |
Zdroj: | Chirality. 2:74-78 |
ISSN: | 0899-0042 |
DOI: | 10.1002/chir.530020203 |
Popis: | Ibuprofen was used to demonstrate that isolated rat hepatocytes offer a suitable in vitro model to investigate the metabolic chiral inversion of anti-inflammatory 2-arylpropionic acids (profens). The inversion of the pharmacologically inactive (-)-(R)-ibuprofen to the active (+)-(S)-ibuprofen was shown to obey apparent first-order kinetics during 5 h and to increase linearly with increasing hepatocyte concentration up to 4 x 10(5) cells/ml. No elimination of (R)-ibuprofen by routes other than inversion was seen, whereas the elimination of (S)-ibuprofen appeared to be saturable. |
Databáze: | OpenAIRE |
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