Effects of COR627 and COR628 on the displacement of [3H]CGP54626 by GABA in rat cortical membranes
Data are means ± S.E.M. from five independent experiments. Best curve fits were obtained with a two-site model (F test; GraphPad Prism) in all cases.
| High-Affinity IC50 | High-Affinity Site | Low-Affinity IC50 | Low-Affinity Site | |
|---|---|---|---|---|
| nM | % | μM | % | |
| GABA | 27.0 ± 10.0 | 44.6 ± 3.3 | 3.4 ± 0.4 | 55.4 ± 3.4 |
| GABA + COR627 (30 μM) | 2.6 ± 1.0* | 39.4 ± 4.3 | 1.8 ± 0.3* | 60.6 ± 4.4 |
| GABA + COR628 (30 μM) | 4.9 ± 1.7* | 45 ± 5.3 | 1.4 ± 0.2** | 54.8 ± 5.4 |