Open dwell times and drug association rates kon
Open times were measured in the presence of a high concentration of the drug. The on-rate kon was calculated from eq. 2 at a drug concentration of 1 μM. Data were obtained from n = 1 to 4 different patches and several hundred to >1,000 events per condition.
| Amiloride | Benzamil | |||
|---|---|---|---|---|
| Mutant | Open Dwell Time | kon | Open Dwell Time | kon |
| ms | μM−1s−1 | ms | μM−1s−1 | |
| wt (αβγ) | 12 ± 1 | 80 ± 8 | 14 ± 2 | 68 ± 6 |
| αS583C | 9.1 | 107 | N.D. | N.D. |
| βG525C | 37 ± 11 | 22 ± 7 | 46 ± 3 | 17 ± 1 |
| αβ | 14 ± 3 | 68 ± 15 | 16 ± 2 | 57 ± 3 |
N.D., not determined.