TABLE 1.
Compound | GABA-Gated Whole-Cell Current |
Tonic Current |
||
---|---|---|---|---|
Allosteric Effect: EF(2-fold GABA)a | Direct Effect: E30 pA | |||
E1 pA | EF(2-fold GABA)a | |||
nM | μMb | μMc | nM | |
AP | 474 | 273.5 | 100.6 | 80 |
GX | 389 | 336.1 | 64.0 | 290 |
GABAd | — | 1426.3 | 19.6 | — |
EF values represent the effective functional concentration of drug (nanomolars) required to double the 3 μM GABA (EC10) response.
E30 μM values represent the mean tonic current responses of drug at 30 μM concentration.
E1 μM values represent the mean tonic current responses of drug at 1 μM concentration co-applied with 1 μM GABA. GABA 1 μM tonic current response: 0.66 ± 0.22 pA/pF, 19.6 pA.
GABA median effective concentration (EC50): 18.6 μM. EC50 values represent the concentration required to produce half of its own maximal effect.