Affinity of the amiloride compounds at the α2A-adrenergic receptor
| Amiloride analogue | 30° | 20° | ||
|---|---|---|---|---|
| n | logKi | n | logKi | |
| Amiloride | 3 | 4.54 ± 0.03 | 2 | 4.52 ± 0.03 |
| BZA | 2 | 5.50 ± 0.05 | 2 | 5.45 ± 0.09 |
| DMA | 4 | 5.64 ± 0.03 | 2 | 5.44 ± 0.01 |
| EPA | 3 | 5.78 ± 0.06 | 2 | 5.78 ± 0.05 |
| MBA | 4 | 6.27 ± 0.05 | 2 | 6.25 ± 0.01 |
| HMA | 6 | 6.78 ± 0.07 | 2 | 6.68 ± 0.01 |
The log affinities were determined in competition equilibrium experiments versus [3H]yohimbine, performed at either 30° for 60 min or 20° for 120 min. The data were fitted with eq. 1, with the slope factor set at 1; then, the derived log apparent affinity constants were converted to the log affinity constants logKi using the Cheng-Prusoff correction. Values are mean ± standard error from n experiments.