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Evidence for a role of cytochrome P450 2D6 and 3A4 in ethylmorphine metabolism.
| Content Provider | Scilit |
|---|---|
| Author | Liu, Z. Mortimer, O. Smith, Ca Wolf, Cr Rane, A. |
| Copyright Year | 1995 |
| Description | Journal: British journal of clinical pharmacology Ethylmorphine is metabolised by N-demethylation (to norethylmorphine) and by O-deethylation (to morphine). The O-deethylation reaction was previously shown in vivo to co-segregate with the O-demethylation of dextromethorphan indicating that ethylmorphine is a substrate of polymorphic cytochrome P450(CYP)2D6. To study further the features of ethylmorphine metabolism we investigated its N-demethylation and O- deethylation in human liver microsomes from eight extensive (EM) and one poor metaboliser (PM) of dextromethorphan. Whereas N-demethylation varied only two-fold there was a 4.3-fold variation in the O- deethylation of ethylmorphine, the lowest rate being observed in the PM. Quinidine, at a concentration of 1 microM, inhibited O-deethylation in microsomes from an EM, but was unable to do so in microsomes from the PM. The immunoidentified CYP2D6 and CYP3A4 correlated with the rates of O-deethylation (r = 0.972) and N-demethylation (r = 0.969), respectively. We conclude that the O-deethylation of ethylmorphine is catalysed by the CYP2D6 in human liver microsomes consistent with previous findings in healthy volunteers. |
| Related Links | http://europepmc.org/articles/pmc1364985?pdf=render https://onlinelibrary.wiley.com/doi/pdf/10.1111/j.1365-2125.1995.tb04413.x |
| Ending Page | 80 |
| Page Count | 4 |
| Starting Page | 77 |
| e-ISSN | 13652125 |
| DOI | 10.1111/j.1365-2125.1995.tb04413.x |
| Journal | British journal of clinical pharmacology |
| Issue Number | 1 |
| Volume Number | 39 |
| Language | English |
| Publisher | Wiley-Blackwell |
| Publisher Date | 1995-01-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: British journal of clinical pharmacology |
| Content Type | Text |
| Resource Type | Article |
