Potency and selectivity in vitro and in vivo
Human Recombinant Enzymes | Human Whole Blood | Rat Air Pouch | |||||||
|---|---|---|---|---|---|---|---|---|---|
| COX-1 | COX-2 | COX-1 | COX-2 | COX-1a | COX-2b | ||||
| μM (±S.D.) | mg/kg | ||||||||
| COX-2 selective | |||||||||
| Valdecoxib | 150 (32) | 0.005 (0.002) | 21.9 (3.5) | 0.2 (0.05) | >200 | 0.06 | |||
| Celecoxib | 15 (3.4) | 0.04 (0.013) | 8.3 (1.4) | 0.3 (0.06) | >200 | 0.2 | |||
| Rofecoxib | >1000 | 0.5 (0.5) | 7.0 (3.33) | 0.2 (0.06) | >200 | 1.1 | |||
| Etoricoxib | >1000 | 5 (4.3) | 11.7 (4.7) | 0.5 (0.08) | 50 | 1.5 | |||
| NSAIDs | |||||||||
| Indomethacin | 0.1 | 1.0 | 0.3 | 0.1 | 0.1 | 0.2 | |||
| Naproxen | 32 | 235 | 9.2 | >100 | 0.1 | 1.3 | |||
| Ibuprofen | 38 | 117 | 3.6 | 10.4 | 0.2 | 2.5 | |||
| Diclofenac | 0.03 | 0.01 | 0.2 | 0.02 | 0.3 | 0.8 | |||
| Etodolac | >100 | 54 | 14 | 0.3 | 0.2 | 5.1 | |||
| Nabumetone | 82 | >1000 | >50 | >50 | 14 | 22 | |||
| Piroxicam | 680 | 660 | 3.7 | 3.5 | 0.1 | 0.9 | |||
| Meloxicam | 1300 | 1700 | 9.5 | 0.3 | 0.7 | 1.0 | |||
| SC-560 | 0.005 | 40 | 0.01 | 0.4 | 0.3 | 12.9 | |||