Pub. Date : 1997 Mar
PMID : 9088578
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Evidence for involvement of human CYP3A in the 3-hydroxylation of quinine. | Quinine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 2 | AIMS: Our previous studies using in vitro hepatic microsomal preparations suggested that the hepatic metabolism of quinine to form the major metabolite 3-hydroxyquinine is most likely catalysed by human P450 3A (CYP3A). | Quinine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 3 | Quinine 3-hydroxylation was inhibited by the specific CYP3A inhibitors, troleandomycin, midazolam and erythromycin. | Quinine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 4 | Competitive inhibition of quinine 3-hydroxylation was observed with a substrate known to be specifically metabolized by human CYP3A, i.e. midazolam, with an apparent Ki value of 11.0 microM. | Quinine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 5 | CONCLUSIONS: The present results strongly indicate that the conversion of quinine to 3-hydroxyquinine is the major metabolic pathway in human liver in vitro and that the reaction is catalysed by CYP3A isoforms. | Quinine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |