TABLE 1.
The efficacy (Imax) and potency (EC50) of acetylcholine and arylidene anabaseines with wild-type and Gln-57 mutant α7 receptors evaluated by net charge. Some compounds only showed a response at 300 μm, whose net charge value is reported as Imax and efficacy is displayed as N/A
| WT |
Q57L |
Q57K |
Q57D |
Q57E |
||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Imax | EC50 | Imax | EC50 | Imax | EC50 | Imax | EC50 | Imax | EC50 | |
| ACh | 1.0 | 31 ± 3 | 1.0 | 26 ± 3 | 1.0 | 65 ± 3 | 1.0 | 18 ± 2 | 1.0 | 36 ± 4 |
| 2FAB | 0.50 ± 0.02 | 16 ± 2 | 0.55 ± 0.04 | 11 ± 2 | 0.29 ± 0.00 | 49 ± 2 | 0.40 ± 0.01 | 6.8 ± 0.6 | 0.35 ± 0.02 | 34 ± 4 |
| 3FAB | 0.13 ± 0.00 | 83 ± 3 | 12% | N/A | 4 ± 1% | N/A | 0.14 ± 0.01 | 45 ± 9 | 4 ± 1% | N/A |
| 2PyroAB | 0.27 ± 0.01 | 5.8 ± 0.9 | 0.14 ± 0.02 | 8.8 ± 3.4 | 0.15 ± 0.01 | 37 ± 8 | 0.44 ± 0.02 | 2.1 ± 0.3 | 0.20 ± 0.01 | 11 ± 2 |
| 3PyroAB | 0.44 ± 0.04 | 17 ± 5 | 0.45 ± 0.02 | 4.7 ± 0.9 | 0.25 ± 0.01 | 28 ± 1 | 0.65 ± 0.03 | 5.4 ± 0.8 | 0.48 ± 0.03 | 4.4 ± 1.1 |
| 2TAB | 0.23 ± 0.02 | 46 ± 9 | 0.17 ± 0.01 | 54 ± 9 | 0.08 ± 0.00 | 101 ± 1 | 0.19 ± 0.02 | 34 ± 9 | 0.15 ± 0.02 | 34 ± 12 |
| 3TAB | 0.25 ± 0.00 | 46 ± 1 | 0.26 ± 0.02 | 15 ± 4 | 0.11 ± 0.00 | 98 ± 5 | 0.34 ± 0.02 | 18 ± 3 | 0.18 ± 0.03 | 38 ± 19 |