Structure-activity relationships for the blockade of T-currents in rat DRG cells and peripheral antinociception by 5α -reduced neuroactive steroids A summary of effects of steroids used in this study on isolated T currents and peripheral thermal nociception.
| Compound Name | T Current Inhibition in DRG Cells (IC50) | nH for T Current Blockade | Peripheral Analgesia (ED50) | nH for Analgesia | Max Increase in PWL |
|---|---|---|---|---|---|
| μM | μg/100 μL | s | |||
| 3βOH | 2.8 ± 0.6 | 1.0 ± 0.2 | 0.03±0.02 | 0.5 ± 0.1 | 5.9 |
| 19-Nor3αCN | 6.0 ± 1.0 | 1.0 ± 0.1 | 0.30±0.20 | 0.8 ± 0.3 | 5.4 |
| 19-Nor3βOH | 6.0 ± 0.6 | 1.0 ± 0.1 | 0.36±0.06 | 0.5 ± 0.1 | 4.55 |
| 19-Nor3βCN | 6.3 ± 0.3 | 1.0 ± 0.1 | 0.16±0.10 | 0.7 ± 0.3 | 3.99 |
| 3αOH | 8.2 ± 0.9 | 1.0 ± 0.1 | 0.24±0.09 | 0.6 ± 0.2 | 5.6 |
| 3αCN | 11 ± 2 | 1.0 ± 0.1 | 0.78±0.50 | 0.8 ± 0.4 | 5.0 |
| 3βCN | 20 ± 10 | 1.0 ± 0.1 | 0.26±0.01 | 0.9 ± 0.1 | 3.5 |
| 19-Nor3αOH | 40 ± 10 | 1.8 ± 0.4 | 1.05±0.40 | 0.6 ± 0.3 | 3.66 |