Potency estimates of GSK-961081 and comparator drugs for relaxation of precontracted guinea pig isolated trachea
For GSK-961081, the MA and BA potencies were obtained by determining relaxation of MCh precontracted tissue (in the presence of propranolol) and histamine precontracted tissue, respectively. The composite MABA potencies were obtained by determining relaxation of MCh precontracted tissue in the absence of propranolol. Data shown are mean (95% confidence interval), n = 6–14.
| Compound | MA | BA | MABA |
|---|---|---|---|
| EC50 (nM) | |||
| GSK-961081 | 50.2 (38.5–65.5) | 24.6 (19.4–31.3) | 11.0 (8.7–13.9) |
| Salmeterol | NA | 98.4 (44.0–219.7) | NA |
| Tiotropium | 1.1 (0.9–1.2) | NA | NA |
NA, not applicable.