Table 3.
Cat whole blood COX-1 and COX-2 inhibitory activities and plasma levels attained following the second, fourth and sixth acetic acid voids for non- and selective COX inhibitors examined
| |
|
|
|
|
|
|
|
Plasma level of drug at acetic acid void (μM) |
||
|---|---|---|---|---|---|---|---|---|---|---|
| Drug | Dose (mg kg−1 i.v.) | COX-1 IC50 (μM) | COX-2 IC50 (μM) | COX-1 IC80 (μM) | COX-2 IC80 (μM) | IC50 ratio | IC80 ratio | 2 | 4 | 6 |
| Ketoprofen |
0.3 |
0.023±3 × 10−4 |
1.18±0.04 |
0.12±0.03 |
3.7±2.4 |
0.019 |
0.03 |
7.81±1.52 |
3.52±1.40 |
1.86±0.78 |
| Indomethacin |
0.3 |
0.13±0.01 |
0.08±2 × 10−3 |
0.41±0.07 |
0.93±0.39 |
1.63 |
0.44 |
1.87±0.46 |
0.99±0.31 |
0.51±0.17 |
| FR-122047 |
1 |
0.07±1 × 10−2 |
0.53±0.01 |
0.37±0.2 |
2.78±1.65 |
0.13 |
0.13 |
0.29±0.07 |
0.18±0.05 |
0.14±0.02 |
| |
3 |
|
|
|
|
|
|
0.32±0.08 |
0.53±0.07 |
0.77±0.02 |
| NS-398 |
1 |
24.0±0.75 |
0.30±8 × 10−3 |
—a |
3.34±2.77 |
80 |
—a |
5.15±1.53 |
3.68±0.75 |
2.62±0.75 |
| |
3 |
|
|
|
|
|
|
19.0±5.46 |
11.4±2.46 |
8.83±1.17 |
| Nimesulide |
1 |
5.69±0.13 |
0.32±8 × 10−3 |
46.0±17.7 |
5.33±2.72 |
18 |
8.6 |
24.9±2.45 |
23.6±1.42 |
19.6±1.14 |
| 3 | 49.9±3.38 | 38.6±1.12 | 56.8±3.43 | |||||||
a
COX-1 IC80 value and ratio for NS-398 could not be determined due to lack of complete inhibition of COX-1.
All values are mean±s.e.m.