Table 1.
Structures of 4AP, 3F4AP, 3CF34AP, 3MeO4AP, 3Me4AP and their pKa, logD, Kv1 and EC50 values.
| drug |
|
|
|
|
|
|---|---|---|---|---|---|
|
| |||||
| pKa | 9.58 | 7.65 | 7.17 | 9.18 | 9.82 |
| logD | −1.478 | 0.414 | 1.484 | −0.76 | −1.232 |
| IC50// M | 293 | 244 | 1061 | 807 | 40 |
| EC50//−M | 59.2 | 96.3 | --a | --a | --a |
(half-maximal inhibitory concentration) is the drug concentration at which 50% of current through Kv1 channels is blocked. EC50 (half-maximal effective concentration) is the drug concentration at which the compound action potential of dysmyelinated nerves increases by 50%. All data in this table were previously reported: pKa, logD, and (Rodriguez-Rangel et al., 2020) and EC50 values (Brugarolas et al., 2018b).
not available.