Table 2.
Analgesic activity of A-803467
| Pain model | ED50 | Effect, % |
|---|---|---|
| Acute nociception | ||
| Rat acute therm. | >100 | 0 ± 0 |
| Rat acute mech. | 65 | 70 ± 4* |
| Inflammatory pain | ||
| Formalin-flinching | >100 | 9 ± 11 |
| Capsaicin, mech. allodynia | 100 | 46 ± 4* |
| CARR, therm. hyperalgesia | 100 | 54 ± 10* |
| CFA, therm. hyperalgesia Day 2 | 41 | 64 ± 6* |
| CFA, therm. hyperalgesia Day 4 | 38 | 71 ± 10* |
| CFA, mech. allodynia Day 2 | >100 | 34 ± 15* |
| CFA, mech. allodynia Day 4 | >100 | 42 ± 15* |
| Neuropathic pain | ||
| SNL, mech. allodynia | 47 | 70 ± 12* |
| CCI, mech. allodynia | 85 | 56 ± 10* |
| CCI, cold allodynia | 70 | 61 ± 11* |
| Vincristine, mech. allodynia | >100 | 9 ± 9 |
| Postoperative pain | ||
| Skin incision at 2 h | >100 | 14 ± 2 |
| Skin incision at 24 h | >100 | 32 ± 18* |
| Visceral pain | ||
| Mouse writhing assay (s.c.) | >100 | 34 ± 6* |
| Cyclophosphamide, cystitis | >100 | 0 ± 10 |
| Colonic distension (MED) | 100 | 25 ± 5* |
| Motor effects† | ||
| Locomotor activity | >300 | 12 ± 12 |
| Rotorod performance | >300 | 0 ± 0 |
| Edge balance | >300 | 0 ± 0 |
Percent analgesic effect assessed at 100 mg/kg, i.p.
*, significantly different (P < 0.05) from vehicle-treated animals (n = 6–12 per experimental group).
†, percent effect tested at 300 mg/kg, i.p. therm., thermal; mech., mechanical; MED, minimum effective dose; CCI, chronic constriction injury, SNL, spinal nerve ligation.