ACh sensitivity of wild-type and mutant neuronal nAChRs
EC50 and nH values were determined by fitting to a Hill equation (see Materials and Methods). Values are the mean ± S.E.M. of data from three to nine oocytes.
| Receptor | EC50 | nH |
|---|---|---|
| μM | ||
| WT α4β4 | 19 ± 4 | 1.3 ± 0.3 |
| α4H2E β4 | 21 ± 7 | 0.9 ± 0.3 |
| α4H2A β4 | 31 ± 11 | 1.1 ± 0.4 |
| α4E59A β4 | 39 ± 10 | 0.8 ± 0.2 |
| α4H61N β4 | 19 ± 4 | 1.2 ± 0.3 |
| α4H104D β4 | 23 ± 5 | 1.0 ± 0.2 |
| α4H104A β4 | 43 ± 10 | 1.3 ± 0.3 |
| α4H109L β4 | 17 ± 5 | 1.4 ± 0.6 |
| α4H162G β4 | 15 ± 2 | 1.6 ± 0.3 |
| α4-2 β4 | 32 ± 6 | 1.1 ± 0.2 |
| α4 β4C75S | 17 ± 3 | 1.5 ± 0.4 |
| α4 β4H157R | 17 ± 3 | 1.2 ± 0.3 |
| α4 β4D195A | 25 ± 3 | 0.9 ± 0.1 |
| α4 β4H469Y | 14 ± 3 | 1.2 ± 0.2 |
| α4E59A, H162G β4 | 25 ± 4 | 1.2 ± 0.2 |
| α4H61N, H162G β4 | 14 ± 8 | 1.0 ± 0.7 |
| α4H162G β4H469Y | 21 ± 4 | 1.0 ± 0.1 |
| α4-2 β4C75S (pseudo-WT) | 34 ± 12 | 0.9 ± 0.3 |
| α4-2E59C β4C75S | 39 ± 7 | 1.7 ± 0.5 |
| α4-2H61C β4C75S | 23 ± 3 | 1.2 ± 0.2 |
| α4-2H162C β4C75S | 21 ± 3 | 1.1 ± 0.1 |
| WT α4β2 | 33 ± 8 | 1.5 ± 0.4 |
| α4E59A β2 | 42 ± 21 | 0.8 ± 0.2 |
| α4H162G β2 | 27 ± 7 | 1.3 ± 0.3 |