Table 1. Obtained PAM EC50 Values for 1 and DS2 at Selected GABAA Receptor Subtypesa.
EC50 (μM) (pEC50 0ESEM, n) |
EC20 (μM) | |||
---|---|---|---|---|
1b | DS2b | GABA | GABA | |
α1β2δ | 3.68 (5.43 ± 0.055, 4) | 2.97 (5.53 ± 0.13, 3) | 6.71 (5.17 ± 0.087, 4) | 1.6–2.0 |
α4β2δ | 2.91 (5.54 ± 0.069, 3) | 1.41 (5.85 ± 0.085, 3) | 0.25 (6.61 ± 0.030, 3) | 0.08 |
α6β2δ | 2.25 (5.65 ± 0.0038, 3) | 2.02 (5.69 ± 0.10, 3) | 0.21 (6.68 ± 0.13, 3) | 0.05 |
α6β2γ2s | no modulation (n = 3) | no modulation (n = 3) | 0.50 (6.30 ± 0.091, 3) | 0.1–0.2 |
GABA agonist EC50 values are given for reference and GABA EC20 used for PAM testing is also given. No modulation means no activity at 10 μM.
Tested as PAMs in the presence of the stated GABA EC20.