Table 2. Inhibition Potency (IC50) of Test Compounds at α7- and α9α10-nAChR Determined from Concentration Response Curves Illustrated in Figure 1.
| α7 IC50 μM (peak current) | α7 IC50 μM (AUC) | α9α10 IC50 μM | |
|---|---|---|---|
| 1a | 1.99 (1.78–2.24) | 2.08 (1.10–3.93) | 6.68 (5.62–7.76) |
| 2 | 1.49 (1.23–1.78) | 2.17 (1.32–3.58) | 36.5 (17.0–77.6) |
| 6 | NA | NA | 9.12 (7.76–10.72) |
| 25 | 25.7 (21.9–30.2) | 26.9 (20.4–35.5) | 115 (41.7–316) |
| 26 | >100 | >100 | 75.9 (61.7–93.3) |
| 27 | 11.2 (9.77–12.9) | 5.54 (4.27–7.18) | 15.8 (11.7–21.4) |
| 28 | 1.78 (1.45–2.29) | 2.25 (1.78–2.85) | 72.4 (31.6–207.0) |
| 29 | 182 (129–257) | 197 (112–347) | 202 (144–288) |
| 30 | 1.91 (1.48–2.45) | 1.95 (1.63–2.34) | 6.46 (5.49–7.49) |
| 31 | 2.01 (1.70–2.34) | 1.86 (1.22–2.81) | 8.13 (6.31–13.2) |
| 33 | 1.07 (0.89–1.29) | 1.12 (0.62–2.03) | 15.9 (11.8–21.4) |
The summary of the test compound antagonist potency (IC50 values) is derived using the concentration response curves illustrated in Figure 1. Details of the protocols used are given in the Experimental Section and Figure 1 (legend). Please note that IC50 values at α7-nAChR were calculated using both peak current and area under the curve (AUC) approaches. Both approaches yielded similar values for all compounds tested. Confidence intervals (95% values) are provided in parentheses, which represent the 95% confidence interval of the mean value. “NA”, not applicable (i.e., agonist-induced function was not inhibited by the coapplication of the test compound even at 100 μM).