TABLE 2.
Pharmacological effects of the novel DM compounds on apparent affinity to GABA in the α1β3γ2L GABAAR
| Compound | Kd,GABA (number of cells), μM | Kd,GABA (DM) (number of cells), μM | Kd,GABA/Kd,GABA (DM) (fold difference) |
|---|---|---|---|
| DM497 | 16.8 ± 1.6 (22) | 0.2 ± 0.2 (16) | 84 |
| DM490 | 16.5 ± 1.2 (15) | 0.2 ± 0.02 (14) | 75 |
| DM492 | 16.5 ± 1.2 (15) | 0.3 ± 0.03 (18) | 63 |
| DM489 | 19.0 ± 1.1 (16) | 2.1 ± 0.2 (12) | 9.1 |
| DM495 | 13.0 ± 1.1 (20) | 1.5 ± 0.1 (15) | 8.4 |
| DM480 | 13.0 ± 1.1 (20) | 4.6 ± 0.4 (16) | 2.9 |
Kd,GABA and Kd,GABA (DM) reflect the apparent binding affinities to GABA in the absence or presence of 100 µM of each tested DM compound. The table gives means ± propagated errors (numbers of cells) for Kd,GABA and Kd,GABA (DM) calculated using eq. (2).