Table 7.
SB-706375 (1 μM) is a selective hU-II antagonist in the rat isolated aorta
| Treatment | EC50 (nM) | Rmax (% 60 mM KCl) |
nH |
|---|---|---|---|
| Phenylephrine | |||
| Vehicle-treated | 19.8±3.1 | 146±6 | 2.19±0.41 |
| SB-706375-treated | 23.6±2.7 | 138±7 | 2.30±0.35 |
| Angiotensin II | |||
| Vehicle-treated | 6.3±1.5 | 38±6 | 2.52±1.17 |
| SB-706375-treated | 8.9±1.9 | 40±12 | 1.85±0.53 |
| Endothelin-1 | |||
| Vehicle-treated | 8.5±1.1 | 153±6 | 2.28±0.35 |
| SB-706375-treated | 8.6±1.3 | 151±7 | 1.84±0.10 |
| KCla | |||
| Vehicle-treated | 15.4±0.9 | 101±7 | 8.27±1.73 |
| SB-706375-treated | 16.9±0.9 | 95±6 | 10.51±1.09 |
Pretreatment of rat isolated aortae with SB-706375 (1 μM) does not affect contractions invoked in the rat isolated aorta by KCl, endothelin-1, angiotensin II or phenylephrine. Values are expressed as mean±s.e.m. (n=4).
a
Contractile responses to KCl are expressed as mM (EC50) and % response to 10 μM noradrenaline (Rmax). SB-706375 treatment did not alter EC50, Rmax or nH values of any spasmogen studied (paired t-test).