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. Author manuscript; available in PMC: 2016 Apr 1.
Published in final edited form as: Neuropharmacology. 2014 Dec 5;91:157–168. doi: 10.1016/j.neuropharm.2014.11.027

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.

a

Data for wild type α3β2 from 32.