Maximum percentage of antagonism or AD50 by pyrazole analogs
| Compound | Dose Range Tested (mg/kg) | SA | % MPE | RT |
|---|---|---|---|---|
| SR141716A | 0.1–3 | 100% (3) | 96% (0.1) | 0.34 (0.26–0.44) |
| 3-Substituent | ||||
| O-852 | N.T. | N.T. | N.T. | N.T. |
| O-889 | 3 | 2% (3) | 40% (3) | 11% (3) |
| O-1043 | 3 and 10 | None (3, 10) | 51% (10) | None (3, 10) |
| O-1269 | 1–10 | 38% (3) | 66% (3) | 43% (1) |
| O-1270 | 1–10 | None (10) | 37% (3) | 26% (1) |
| O-1271 | 3 and 10 | 77% (10) | 65% (10) | 36% (3) |
| 1-Substituent | ||||
| O-1253 | 0.1–10 | 97% (1) | 3.3 (1.9–6.0) | 4.7 (2.6–8.3) |
| O-1254 | 10 and 30 | Stimulation | 52% (30) | 31% (10) |
| O-1255 | 10 | 0% (10) | 13% (10) | 14% (10) |
| 5- and/or 4-Substituent | ||||
| O-1302 | 0.1–30 | 91% (1) | 6.4 (2, not available) | 8.6 (4.4–16.4) |
| O-1690 | 0.1–10 | 65% (1) | 1.8 (0.6–5.3) | 2.7 (1.5–4.7) |
| O-1691 | 0.1–10 | 6% (0.3) | 1.9 (1.1–3.2) | 1.8 (1.2–2.7) |
| O-1704 | 0.1–30 | 65% (3) | 1.8 (0.7–4.3) | 2.1 (1.0–4.3) |
| O-1710 | 0.3–10 | 50% (3) | 62% (10) | 51% (1) |
AD50 values expressed as μmol/kg (with 95% confidence limits in parentheses) are provided whenever % antagonism is dose-responsive. When % antagonism was not dose-responsive, values are expressed as maximum % antagonism across all doses tested. Dose(s) (mg/kg) at which the maximum antagonist effect occurred are given in parentheses. For SA, stimulation (i.e., maximum antagonism >100%) was not included in % antagonism calculations.
SA, suppression of spontaneous activity; MPE, % maximum possible antinociceptive effect in tail-flick assay; RT, rectal temperature; N.T., not tested.