Table 1. Comparative Boltzmann Parameters of Voltage-Dependence of Channel Activation Curves for the Respective Affinity Bait Reagentsa.
| condition | concentration | V1/2 | k |
|---|---|---|---|
| control | –12.8 ± 0.5 (4) | 7.4 ± 0.5 (4) | |
| (R)-8 | 30 nM | –12.3 ± 0.8 (5) | 6.6 ± 0.7 (5) |
| 100 nM | –12.9 ± 0.3 (5) | 6.7 ± 0.3 (5) | |
| 300 nM | –9.7 ± 0.7 (4) | 7.3 ± 0.6 (4) | |
| 1 μM | –11.3 ± 0.5 (5) | 7.5 ± 0.4 (5) | |
| 3 μM | –12.2 ± 0.5 (6) | 7.1 ± 0.5 (6) | |
| (S)-8 | 300 nM | –10.8 ± 0.4 (4) | 6.9 ± 0.4 (4) |
| 1 μM | –6.9 ± 0.4 (5)* | 7.1 ± 0.3 (5) | |
| 3 μM | –9.1 ± 0.6 (5) | 6.4 ± 0.5 (5) | |
| 10 μM | –9.3 ± 0.4 (4) | 7.1 ± 0.3 (4) | |
| 30 μM | –13.7 ± 0.6 (5) | 6.8 ± 0.5 (5) | |
| (R)-9 | 300 pM | –16.9 ± 1.0 (4) | 6.2 ± 0.7 (4) |
| 1 nM | –20.8 ± 2.0 (4)* | 8.4 ± 1.5 (4) | |
| 100 nM | –12.6 ± 1.8 (4) | 10.0 ± 1.3 (4) | |
| 1 μM | –15.0 ± 0.6 (2) | 6.2 ± 0.6 (2) | |
| (R)-10 | 3 μM | –13.0 ± 0.5 (4) | 6.8 ± 0.4 (4) |
| 30 μM | –14.5 ± 1.0 (5) | 6.3 ± 0.5 (5) | |
| 100 μM | –13.9 ± 1.4 (5) | 6.8 ± 1.1 (5) | |
| 300 μM | –13.8 ± 1.7 (4) | 6.9 ± 1.0 (4) |
a
Values for V1/2, the half-maximal activation, and the slope factors (k) were derived from Boltzmann distribution fits to the individual recordings and averaged to determine the mean and standard error (± SEM) displayed above. Asterisk (∗) indicates statistical significance (p < 0.05) compared to control values (one-way ANOVA with Tukey’s posthoc test).