Table 1.
Agonist and modulator activation involve the β2 C loop
Subtype | ACh Activation | ACh + Mor Modulation | ACh + Oxa Modulation | |||||
---|---|---|---|---|---|---|---|---|
EC50 (µM) | nH | EC50 (µM) | nH | Emax | EC50 (µM) | nH | Emax | |
α3β2a | 66 ± 9 | 0.75 ± 0.07 | 10 ± 2 | 1.37 ± 0.80 | 2.64 ± 0.29 | 9 ± 1 | 1.54 ± 0.25 | 2.27 ± 0.06 |
α3Y168C· β2D190C |
37 ± 6 | 0.68 ± 0.08 [10] |
2.9 ± 0.6 | 1.22 ± 0.33 [4–5] |
1.37 ± 0.06 | 9.5 ± 4.0 | 1.13 ± 0.45 [5] |
1.38 ± 0.11 |
α3Y168Cβ2 | 36 ± 8 | 0.70 ± 0.11 [11] |
1.6 ± 0.6 | 1.17 ± 0.47 [6] |
1.46 ± 0.08 | 5.9 ± 1.6 | 1.01 ± 0.27 [6] |
1.34 ± 0.06 |
α3β2D190C | 12 ± 2 | 1.05 ± 0.14 [9] |
19 ± 8 | 1.08 ± 0.42 [4] |
0.95 ± 0.08 | 31 ± 12 | 1.13 ± 0.44 [5] |
0.83 ± 0.08 |
α3Y168Fβ2 | 14 ± 2 | 0.61 ± 0.04 [12] |
0.14 ± 0.03 | 0.50 ± 0.08 [6] |
1.15 ± 0.03 | 2.9 ± 0.2 | 1.73 ± 0.66 [6] | 1.16 ± 0.02 |
α3β2D190Q | 12 ± 2 | 1.00 ± 0.15 [8] |
13 ± 6 | 0.73 ± 0.25 [4] |
1.20 ± 0.11 | 31 ± 5 | 1.19 ± 0.21 [4] | 0.97 ± 0.04 |
α3Y168F β2D190Q |
46 ± 7 | 0.83 ± 0.09 [11] |
4.0 ± 1.2 | 1.17 ± 0.33 [4] |
2.57 ± 0.14 | 10 ± 1 | 1.10 ± 0.09 [4] | 1.06 ± 0.02 |
Fits to the Hill equation for experiments with ACh alone, ACh +10 µM Mor or ACh +10 µM Oxa. In all experiments for the α3Y168Cβ2D190C double mutant, recordings were made on naive oocytes, having had no previous oxidation or reduction treatment [n] indicates the number of replicate oocytes for each measurement.
Data for wild type α3β2 from 32.