Effect of different compounds on metabolism of meloxicam by human liver microsomes: influence of sulfaphenazole
| Activator | Activity As % of Control | |||
|---|---|---|---|---|
| Minus Sulfaphenazole | Plus Sulfaphenazole | |||
| 10 μM | 100 μM | 10 μM | 100 μM | |
| Control | 100 | 100 | 100 | 100 |
| Quinine | 130 | 200 | 200 | 610 |
| Quinidine | 140 | 280 | 330 | 940 |
| Cinchonine | 110 | 160 | n.d. | n.d. |
| Cinchonidine | 120 | 140 | n.d. | n.d. |
| Quinuclidine | 100 | 110 | 84 | 41 |
| Chloroquine | 100 | 130 | n.d. | n.d. |
| Hydroquinidine | 210 | 480 | 520 | 2100 |
| Hydroxyquinuclidine | 100 | 110 | n.d. | n.d. |
| Primaquine | 100 | 60 | n.d. | n.d. |
| Hydroxychloroquine | 110 | 130 | 140 | 170 |
| α-Naphthoflavone | 84 | 1 | 130 | 43 |
| Papaverine | 83 | 30 | 110 | 63 |
Meloxicam (10 μM) was incubated in 0.1 M Tris buffer, pH 7.4, at 37°C with human liver microsomes (0.5 mg of protein/ml), an NADPH-generating system (consisting of 1.2 mM NADP, 0.7 U of glucose 6-phosphate dehydrogenase/ml, 8 mM glucose 6-phosphate, and in the presence of different compounds at two concentrations (10 and 100 μM) and with (control, 4.8 pmol/min/mg protein) and without (control, 12.3 pmol/min/mg protein) sulfaphenazole (10 μM) for 30 min (mean of duplicate experiments). n.d., not determined.