Table 2.
Pharmacological parameters for 5Me3F4AP, 3F4AP, 4AP and 3Me4AP.
Drug | pKa | logD (pH 7.4) | Pe (nm/s) |
---|---|---|---|
5Me3F4AP | 7.46 ± 0.01 | 0.664 ± 0.005 | 43.3 ± 0.5 |
4AP | 9.19 ± 0.03 | −1.478 ± 0.014a | 2.36 ± 0.03b |
3F4AP | 7.37 ± 0.07 | 0.414 ± 0.002a | 13.6 ± 0.5c |
3Me4AP | 9.82 ± 0.06a | −1.232 ± 0.008a | -- |
logD: experimental partition coefficient octanol: water at pH 7.4 (n =4).
pKa: experimental titration coefficient at room temperature (n =3).
Pe: permeability rate across the artificial membrane (n = 2).
previously reported data using the equipment and protocol (Rodriguez-Rangel et al., 2020).
previously reported data (Brugarolas et al., 2018b).
result obtained during the present study, a value of 15.6 ± 0.6 nm/s was previously reported (Brugarolas et al., 2018b).