Summary of pharmacological properties of wild-type and mutant nAChRs
| AChR | ACh Response | Nicotine Response | Efficacy | |||||
|---|---|---|---|---|---|---|---|---|
| α Subunit | β Subunit | Oocytes | EC50 | Hill Coefficient | Oocytes | EC50 | Hill Coefficient | |
| μM | μM | |||||||
| α 4 | β 2 | 6 | 3.3 ± 0.6 | 0.7 ± 0.1 | 4 | 3.9 ± 2.6 | 0.9 ± 0.3 | 100 ± 15 |
| α 4(C226F), M1 | β 2 | 6 | 23 ± 3 | 0.7 ± 0.1 | 5 | 10 ± 1.6 | 0.9 ± 0.1 | 100 ± 12 |
| α 4(L258V), M2 | β 2 | 5 | 2.1 ± 0.4 | 0.7 ± 0.1 | 3 | 2.8 ± 1.2 | 0.8 ± 0.2 | 51 ± 5 |
| α 4(I262T), M2 | β 2 | 3 | 3.5 ± 0.9 | 0.8 ± 0.1 | 2 | 0.30 ± 0.1 | 0.6 ± 0.1 | 23 ± 1.9 |
| α 3 | β 2 | 2 | 130 ± 30 | 1.0 ± 0.2 | 6 | 18 ± 5.6 | 1.1 ± 0.1 | 64 ± 5.6 |
| α 3 | β 2(I224T, S226L), M1 | 4 | 410 ± 120 | 1.2 ± 0.3 | 3 | 190 ± 23 | 2.0 ± 0.4 | 65 ± 3.6 |
| α 3 | β 2(V254F), M2 | 3 | 54 ± 5 | 1.1 ± 0.1 | 3 | 61 ± 20 | 0.8 ± 0.2 | 82 ± 7.7 |
| α 3(V258L), M2 | β 2 | 3 | 83 ± 7 | 1.1 ± 0.1 | 3 | 80 ± 4.8 | 1.0 ± 0.1 | 100 ± 2.0 |
| α 3(T262I), M2 | β 2 | 3 | 48 ± 7 | 1.0 ± 0.1 | 4 | 8.2 ± 1.7 | 1.0 ± 0.2 | 55 ± 3.1 |
| α 3 | β 4 | 3 | 310 ± 40 | 2.1 ± 0.7 | 4 | 330 ± 24 | 1.5 ± 0.1 | 76 ± 2.1 |