Effects of SB 209670, BQ-788, RES-701 or BQ-123 against contractions produced by ET-1, ET-3, S6c, BQ-3020 or IRL 1620 in human bronchus
| Compound | pKB | ||||
|---|---|---|---|---|---|
| ET-1 | ET-3 | S6c | BQ-3020 | IRL 1620 | |
| SB 209670 | 6.1 (11) | N.E. (6) | 6.4 (13) | 8.02-a (6) | 8.4 (5) |
| (3 μM) | (3 μM) | (3 μM) | (0.3 μM) | (0.3 μM) | |
| BQ-788 | N.E. (5) | N.E. (5) | N.E. (9) | 7.7 (8) | 7.8 (6) |
| (3 μM) | (3 μM) | (3 μM) | (0.3 μM) | (0.3 μM) | |
| RES 701 (all 10 μM) | L.S. (6) | N.E. (6) | N.E. (4) | N.E. (5) | N.E. (4) |
| BQ-123 (all 3 μM) | N.E. (6) | N.E. (4) | N.E. (5) | 6.2 (7) | N.D. (4) |
Results are expressed as pKB; the n values and antagonist concentrations are given in parentheses. N.E., No effect. L.S., Potentiation, reflected by leftward shift in the concentration-response curve.
↵2-a Estimated pKB, as there was a marked reduction in the agonist-induced maximum response.