EC50 and Imax values of ACh, choline, 4OH-GTS-21, and AR-R17779 in wild-type and mutant α7 and α4β2 receptors
| Drug | Receptor | EC50 ± S.E.M. | Imax ± S.E.M. Relative to ACh Maximum | Imax ± S.E.M. Relative to Wild-Type ACh Maximum |
|---|---|---|---|---|
| ACh | α7 | 31 ± 4 | 1 | 1 |
| α7W55A | 85 ± 6 | 1 | 2.5 ± 0.4 | |
| α7W55F | 33 ± 3 | 1 | 0.5 ± 0.1 | |
| α7W55G | 602 ± 35 | 1 | 2.4 ± 0.25 | |
| α7W55V | 84 ± 2.5 | 1 | 1.2 ± 0.1 | |
| α7W55YY | 30 ± 5 | 1 | 0.6 ± 0.2 | |
| α7W149A | 194 ± 10 | 1 | 0.15 ± 0.03 | |
| α7W149G | 400 ± 19 | 1 | 0.17 ± 0.03 | |
| α4β2 | 76 ± 20 | 1 | 1 | |
| α4β2W57A | 468 ± 59 | 1 | 0.09 ± 0.01 | |
| α4β2W57F | 33 ± 4 | 1 | 0.04 ± 0.02 | |
| α4β2W57G | 47 ± 11 | 1 | 0.08 ± 0.02 | |
| α4β2W57V | 87 ± 10 | 1 | 0.05 ± 0.013 | |
| α4β2W57Y | 16 ± 2 | 1 | 0.08 ± 0.03 | |
| α4W154A β2 | 526 ± 28 | 1 | 0.40 ± 0.04 | |
| α4W154F β2 | 118 ± 6 | 1 | 0.39 ± 0.06 | |
| α4W154Y β2 | 81 ± 3 | 1 | 0.04 ± 0.00 | |
| Choline | α7 | 304 ± 21 | 0.90 ± 0.02 | 0.90 ± 0.02 |
| α7W55A | 950 ± 210 | 0.95 ± 0.05 | 2.3 ± 0.1 | |
| α7W55F | 500 ± 72 | 1.4 ± 0.07 | 0.73 ± 0.04 | |
| α7W55G | >5000 | 1.3 ± 0.12 | >1.5 | |
| α7W55V | 570 ± 12 | 1.1 ± 0.01 | 1.4 ± 0.1 | |
| α7W55Y | 228 ± 13 | 0.84 ± 0.01 | 0.48 ± 0.01 | |
| α7W149A | 2490 ± 130 | 0.89 ± 0.03 | 0.13 ± 0.01 | |
| α7W149G | 6870 ± 1440 | 0.61 ± 0.07 | 0.10 ± 0.02 | |
| 4OH-GTS-21 | α7 | 3.0 ± 0.3 | 0.46 ± 0.01 | 0.46 ± 0.01 |
| α7W55A | 8.4 ± 0.7 | 0.33 ± 0.01 | 0.82 ± 0.02 | |
| α7W55F | 19 ± 2 | 0.45 ± 0.02 | 0.23 ± 0.01 | |
| α7W55G | N.A.* | N.A.* | N.A.* | |
| α7W55V | 7.8 ± 0.8 | 0.94 ± 0.03 | 0.54 ± 0.02 | |
| α7W55Y | N.A.* | N.A.* | N.A.* | |
| α7W149A | 4.5 ± 1.4 | 0.28 ± 0.04 | 0.04 ± 0.01 | |
| α7W149G | 4.4 ± 0.5 | 0.76 ± 0.08 | 0.13 ± 0.02 | |
| α4β2 | N.A.* | 0.01 ± 0.00 | 0.01 ± 0.005 | |
| α4β2W57A | 2.6 ± 0.3 | 0.71 ± 0.02 | 0.07 ± 0.01 | |
| α4β2W57F | 0.66 ± 0.22 | 0.62 ± 0.05 | 0.02 ± 0.002 | |
| α4β2W57G | 1.2 ± 0.2 | 0.74 ± 0.04 | 0.06 ± 0.01 | |
| α4β2W57V | 3.00 ± 0.14 | 0.07 ± 0.01 | 0.0035 ± 0.0005 | |
| α4β2W57Y | 0.65 ± 0.09 | 2.7 ± 0.1 | 0.19 ± 0.01 | |
| AR-R17779 | α7 | 3.60 ± 0.73 | 1.05 ± 0.05 | 1.05 ± 0.05 |
| α7W55A | 32.4 ± 1.7 | 0.96 ± 0.02 | 2.36 ± 0.05 | |
| α7W55F | 82.3 ± 2.5 | 1.02 ± 0.01 | 0.53 ± 0.01 | |
| α7W55G | 332 ± 2 | 0.99 ± 0.04 | 2.36 ± 0.10 | |
| α7W55V | 94 ± 6 | 1.05 ± 0.04 | 1.26 ± 0.05 | |
| α7W55Y | 87 ± 42 | 0.90 ± 0.16 | 0.51 ± 0.09 | |
| α7W149A | 120 ± 4 | 1.07 ± 0.14 | 0.16 ± 0.02 | |
| α7W149G | 506 ± 72 | 0.97 ± 0.09 | 0.17 ± 0.02 |