Receptor type | EC50ACh (μm) | IC50Zn2+ (μm) | nHill | Voltage dependency | n |
---|---|---|---|---|---|
(α4)2(β2)3 | 4.04 ± 0.3 | 19 ± 6 | 0.45 ± 0.014 | Y | 10 |
α4H195Aβ2 | 3.80 ± 0.2 | 156 ± 11* | 0.41 ± 0.03 | Y | 5 |
α4E92Aβ2 | 5.20 ± 0.4 | 51 ± 10* | 0.40 ± 0.02 | Y | 5 |
α4β2D218A | 1.01 ± 0.4 | 160 ± 14* | 0.48 ± 0.01 | Y | 5 |
α4β2D217A | 4.50 ± 0.3 | 17 ± 9 | 0.43 ± 0.03 | Y | 5 |
α4H195Aβ2D218A | 7.01 ± 1.5 | 1144 ± 54* | 0.54 ± 0.01 | Y | 5 |
α4H195Aβ2D217A | 10.0 ± 1.6 | 101 ± 23* | 0.42 ± 0.09 | Y | 5 |
α4H195A,E92Aβ2 | 6.70 ± 1.6 | 156 ± 42* | 0.51 ± 0.07 | Y | 5 |
α4β2D218A,D217A | 4.04 ± 1.2 | 390 ± 20* | 0.48 ± 0.05 | Y | 4 |
α4 E92Aβ2D218A | 3.50 ± 0.9 | 600 ± 99* | 0.45 ± 0.01 | Y | 4 |
α4 E92Aβ2D217A | 4.5 ± 1 | 48 ± 9* | 0.44 ± 0.01 | Y | 4 |
α4H195A,E92Aβ2D218A | 7.86 ± 0.9 | 980 ± 27* | 0.63 ± 0.02* | Y | 5 |
α4β2H71A | 2.30 ± 0.9 | 19 ± 5 | 0.52 ± 0.02* | N | 4 |
α4β2E74A | 4.50 ± 0.8 | 19 ± 7 | 0.65 ± 0.07* | N | 4 |
α4β2D293A | 8.30 ± 2.2 | 21 ± 9 | 0.63 ± 0.02* | N | 3 |
α4β2H71A,E74A | 6.78 ± 0.8 | 17 ± 2 | 0.60 ± 0.02* | N | 4 |
α4β2H71A,E74A,D293A | 5.01 ± 0.7 | 12 ± 4 | 0.60 ± 0.03* | N | 4 |
α4H195Aβ2H71A,E74A | 4.87 ± 0.7 | 178 ± 23* | 0.65 ± 0.04* | N | 4 |
α4H195Aβ2H71A,E74A,D293A,D218A | 4.40 ± 0.9 | 1085 ± 100* | 0.64 ± 0.07* | N | 4 |
α4E224Aβ2 | 4.10 ± 0.3 | 18 ± 6 | 0.41 ± 0.04 | Y | 3 |
α4E228Aβ2 | 4.40 ± 0.6 | 19 ± 5 | 0.43 ± 0.08 | Y | 3 |
α4E224Hβ2 | 3.6 ± 0.2 | 20 ± 7 | 0.52 ± 0.1 | Y | 3 |
α4H195Eβ2 | 4.9 ± 0.9 | 22.04 ± 5 | 0.47 ± 0.09 | Y | 3 |
α4H195E,E224Hβ2 | 4.9 ± 0.8 | 19 ± 11 | 0.51 ± 0.1 | Y | 3 |
The values indicate the ACh EC50 values for activating wild-type and mutant (α4)2(β2)3 nAChRs and also the Zn2+ IC50 values for inhibiting the EC20 ACh responses. All values are means ± SEM from n cells. ND, Not determined.
↵*p < 0.05 compared with (α4)2(β2)3(see Materials and Methods).