Table 4.
Potency of compounds for inhibition of subtypes of nAChRs
| α6/3β2β3V273S | α4β2 | α3β4 | α7 | α1β1δε | |
|---|---|---|---|---|---|
| Compound | pIC50 | pIC50 | pIC50 | pIC50 | pIC50 |
| 1 | 6.9 ± 0.3 | 5.5 ± 0.09 | 5.1 ± 0.05 | 5.3 ± 0.1 | 5.3 ± 0.08 |
| 2 | 6.3 ± 0.05 | 4.9 ± 0.07 | <4.7 | <4.7 | 5.1 ± 0.2 |
| 3 | 6.1 ± 0.1 | 4.8 ± 0.03 | 5.1 ± 0.3 | 5.0 ± 0.01 | 5.2 ± 0.1 |
| 4 | 6.4 ± 0.1 | 4.8 ± 0.08 | 5.1 ± 0.09 | <4.7 | <4.8 |
| 5 | 6.4 ± 0.06 | 6.3 ± 0.2 | 5.5 ± 0.07 | <4.8 | 5.4 ± 0.2 |
| 6 | 6.2 ± 0.03 | 5.7 ± 0.05 | 5.2 ± 0.06 | <4.85 | 5.2 ± 0.06 |
Compounds did not activate any nAChR subtype up to 20 µM (pEC50 < 4.7).
EC50, concentration giving 50% of maximal activation; IC50, concentration giving 50% of maximal inhibition. Results are the mean ± SEM of at least 2 experiments.