Table 3.
In vitro and in vivo activities of target and reference compounds.
| Compound | pA2a | pA10a | Mode of antagonism | Maximum decrease in MABPa,b |
|---|---|---|---|---|
| 4a | 6.7 | 6.1 | C | 51.4 ± 6.1 |
| 4b | 6.9 | 6.3 | C | 52.5 ± 3.4 |
| 4c | 7.1 | 6.2 | C | 49.9 ± 4.8 |
| 4d | 7.1 | 6.4 | C | 50.2 ± 5.9 |
| 4e | 7.2 | 6.3 | C | 51.7 ± 3.1 |
| 4f | 7.0 | 6.2 | C | 47.6 ± 6.4 |
| 4g | 8.4 | 5.4 | NC | 62.4 ± 4.5c,d,e |
| 4h | 7.9 | 5.7 | NC | 64.4 ± 3.9c,d,e |
| 5 | 6.6 | 5.8 | C | 44.7 ± 6.1 |
| 1 | 8.5 | 6.7 | NC | 55.9 ± 3.4 |
| Losartan | 8.0 | 7.1 | C | 58.3 ± 5.6 |
| Candesartan | 8.5 | 6.7 | NC | 56.2 ± 6.3 |
a
n = 6.
b
Dose is 3.0 mg kg−1 except for losartan and candesartan (5.0 mg kg−1).
c
p < 0.05 versus 1.
d
p < 0.05 versus losartan.
e
p < 0.05 versus candesartan.