Inhibitors of M1 and/or M2 formation from tramadol by pooled dog liver microsomes categorized by inhibition potency
Inhibitors are listed according to whether they decrease the indicated activities by at least 50% (compared with no inhibitor added) at 1 µM inhibitor concentration and/or also at 100 µM inhibitor concentration. Inhibitors are also grouped by whether they inhibit M1 formation only, M2 formation only, or both M1 and M2 formation by at least 50% at that inhibitor concentration. The inhibition data used are shown in Table 1.
| Compounds Inhibiting M1 Formation (Only) by >50% | Compounds Inhibiting Both M1 and M2 Formation by >50% | Compounds Inhibiting M2 Formation (Only) by >50% |
|---|---|---|
| Inhibitor concentration: 1 µM | ||
| Bupivacaine | Atipamezole | Fluconazole |
| Citalopram | Desipramine | |
| Imipramine | Levomedetomidine | |
| Ketoconazole | Paroxetine | |
| Maropitant | ||
| Quinidine | ||
| Trifluoperazine | ||
| Inhibitor concentration: 100 µM | ||
| Acepromazine | Amytriptylline | Artemisinin |
| Chloramphenicol | Atipamezole | Carprofen |
| Cimetidine | Bupivacaine | Dexmedetomidine |
| Curcumin | Buprenorphine | Fluconazole |
| Dopamine | Bupropion | Propofol |
| Fentanyl | Citalopram | Selegiline |
| Firocoxib | Clopidrogel | |
| Fluoxetine | Chloramphenicol | |
| Lorazepam | Deracoxib | |
| Maropitant | Desipramine | |
| Metoclopramide | Dextromethorphan | |
| Omeparazole | Diazepam | |
| Oxazepam | Doxepin | |
| Phenacetin | Diphenhydramine | |
| Quinidine | Efavirenz | |
| Terbinafine | Fluconazole | |
| Trazadone | Fluoxetine | |
| Vinblastine | Imipramine | |
| Ketamine | ||
| Ketoconazole | ||
| Ketotifen | ||
| Levomedetomidine | ||
| Methadone | ||
| Midazolam | ||
| Paroxetine | ||
| Quinine | ||
| Trifluoperazine | ||
| Xylazine |