ED50 values (95% confidence limits; milligrams per kilogram) of R116301 and reference NK1 receptor antagonists for inhibition of SP-induced thumping in gerbils
| Compound | Route | Time | ED50 (95% Confidence Limits) |
|---|---|---|---|
| h | mg/kg | ||
| R116301 | i.p. | 0.5 | 0.16 (0.076–0.33) |
| p.o. | 1 | 0.32 (0.18–0.56) | |
| Aprepitant | i.p. | 0.5 | 0.12 (0.060–0.26) |
| p.o. | 1 | 0.20 (0.092–0.44) | |
| GR-203040 | i.p. | 0.5 | 0.16 (0.092–0.28) |
| p.o. | 1 | 1.3 (0.60–2.6) | |
| L-760735 | i.p. | 1 | 1.0 (0.48–2.1) |
| p.o. | 1 | 2.5 (1.2–5.3) | |
| CP-96345 | i.p. | 0.5 | 5.0 (2.1–12) |
| p.o. | 1 | ≥40 | |
| CP-99994 | i.p. | 0.5 | 6.3 (3.0–13) |
| p.o. | 1 | >40 | |
| CGP-49823 | i.p. | 0.5 | 13 (7.2–22) |
| p.o. | 1 | >40 | |
| MDL-103392 | i.p. | 0.5 | >10 |
| p.o. | 1 | >40 | |
| Nolpitantium | i.p. | 0.5 | >40 |