Table 2.
Subtype | ACh Activation | ACh + Mor Modulation | Mor Activation | |||||
---|---|---|---|---|---|---|---|---|
EC50 (µM) | nH | EC50 (µM) | nH | Eax | EC50 (µM) | nH | Emax | |
α3β2a | 66 ± 9 | 0.75 ± 0.07 [5–11] | 10 ± 2 | 1.37 ± 0.80 | 2.64 ± 0.29 [5] | 20 ± 2b | 3.1 ± 1.6 | 0.20 ± 0.04 |
α3S125Yβ2 | 7.6 ± 2.1 | 0.84 ± 0.19 [3–6] | 8.8 ± 4.9nM | 0.31 ± 0.05 | 1.41 ± 0.11 [3–6] | 2.3 ± 0.7 | 1.58 ± 0.42 [3–4] |
1.69 ± 0.27 |
α3S125Y· β2W149A |
4.5 ± 1.4 | 0.61 ± 0.10 [6] |
4.9 ± 2.0 | 0.72 ± 0.16 [5] |
1.33 ± 0.10 | 25 ± 9 | 1.01 ± 0.29 [5–6] |
0.21 ± 0.02 |
α3β2W149A a | 40 ± 6 | 0.99 ± 0.12 [5] | 44 ± 6 | 1.38 ± 0.19 | 0.86 ± 0.03 [5] | N.F. | N.F. | 0.015 ± 0.004 [3] |
α3S125C· β2Q39C |
1.1 ± 0.2 | 0.66 ± 0.09 [3–7] |
0.75 ± 0.40 | 0.62 ± 0.18 [4] |
2.57 ± 0.17 | 0.53 ± 0.21 | 0.92 ± 0.30 [4–8] |
1.00 ± 0.14 |
α3S125Cβ2 | 3.5 ± 1.3 | 0.64 ± 0.13 [5–7] | 0.71 ± 0.20 | 0.85 ± 0.17 | 1.48 ± 0.07 [5] | 92 ± 33 | 0.54 ± 0.11 [4] |
0.028 ± 0.006 |
α3β2Q39C | 130 ± 30 | 0.78 ± 0.12 [4] | 2.0 ± 0.4 | 0.91 ± 0.15 | 2.54 ± 0.09 [6] | N.D. |
Fits to the Hill equation for experiments with ACh alone, ACh + 10 µM Mor or Mor alone. In all experiments for the (α3S125Cβ2Q39C 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. N.F. indicates no fit was possible for data collected in experiment; N.D. indicates no data were collected for experiment.
Data of ACh and ACh + Mor titrations for wild type α3β2, and all data α3β2W149A from 32.
Data of Mor titration for wild type α3β2 from 38.