Modulation by BZ ligands of GABAA receptors expressed inX. laevis oocytes
| Subunit combination | Flunitrazepam | β-CCM 100 nm | CL 218 872 1 μm | Zolpidem 1 μm | |
|---|---|---|---|---|---|
| 100 μm | 1 μm | ||||
| α1β1γ2 | 94.6 ± 20.1 | 108.6 ± 8.9 | −43.8 ± 9.6 | 58.0 ± 6.5 | 140 ± 14 |
| α1β1γ1 | −5.8 ± 3.5 | −10.0 ± 5.5 | −0.9 ± 1.9 | 1.9 ± 2.3 | 2.4 ± 2.3 |
| α1β1γ1ΔI79F | 25.0 ± 5.0 | 68.7 ± 14.8 | −14.0 ± 3.8 | 28.4 ± 4.5 | 0.75 ± 1.4 |
| α1β1γ1ΔL132M | −10.6 ± 2.2 | −14.8 ± 1.7 | 0.1 ± 2.2 | −1.3 ± 0.75 | 0.3 ± 1.3 |
| α1β1γ2ΔF77I | 9.0 ± 1.8 | 11.1 ± 2.3 | −6.5 ± 3.4 | 0.1 ± 4.8 | −1.5 ± 4.1 |
Data represent the percent modulation of a submaximal (EC20) response to GABA by the BZ ligand; each value is the mean ± standard error from at least four individual oocytes. A positive value represents an agonist-like effect and a negative value represents an inverse-agonist effect. A value of zero represents no modulatory effect.