Skip to main content
. 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 2.

Allosteric modulation involves the canonical agonist interface

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.

a

Data of ACh and ACh + Mor titrations for wild type α3β2, and all data α3β2W149A from 32.

b

Data of Mor titration for wild type α3β2 from 38.