α7 Mutation | NS6740 + PNU-120596 (10 µM) | |||||
---|---|---|---|---|---|---|
pEC50 (±S.E.) | EC50 | Hill (±S.E.) | Imax | Fold Shift from WT | n | |
nM | µA | |||||
WT | 7.208 ± 0.031 | 62 | 1.9 ±0.21 | 0.24–2.4 | — | 13 |
TyrA | ||||||
TyrOMe | 8.445 ±0.023 | 3.6 | 3 ±0.41 | 0.33–34 | 0.06 | 10 |
3-F1TyrOMe | 8.035 ±0.053 | 9.2 | 2 ±0.41 | 0.19–25 | 0.15 | 11 |
3,5-F2TyrOMe | 7.918 ±0.051 | 12 | 2 ±0.41 | 0.43–39 | 0.2 | 12 |
4-BrPhe | 8.145 ±0.025 | 7.2 | 2.7 ±0.31 | 0.13–25 | 0.12 | 13 |
4-CNPhe | 7.146 ±0.017 | 71 | 3.1 ±0.27 | 2.9–32 | 1.2 | 13 |
2,3,5,6-F4TyrOMe | 5.883 ±0.038 | 1300 | 3.4 ±0.74 | 0.01–1.6 | 21 | 10 |
Phe | 8.041 ±0.019 | 9.1 | 2.9 ±0.34 | 1.2–16 | 0.15 | 14 |
4-MePhe | 7.92 ±0.02 | 12 | 2.5 ±0.28 | 0.01–0.29 | 0.19 | 13 |
4-F1Phe | 6.72 ±0.017 | 190 | 2.1 ±0.15 | 0.13–2.7 | 3.1 | 13 |
TrpB | ||||||
Trp | 7.182 ±0.023 | 66 | 2.4 ±0.25 | 0.06–0.46 | 1.1 | 13 |
F3Trp | 6.466 ±0.013 | 340 | 2.3 ±0.12 | 0.02–6.8 | 5.5 | 14 |
TyrC2 | ||||||
Phe | 7.218 ±0.072 | 60 | 2 ±0.33 | 0.01–0.41 | 0.96 | 13 |
TyrOMe | 7.344 ±0.029 | 46 | 2.2 ±0.26 | 0.01–0.08 | 0.74 | 10 |
4-F1Phe | 7.069 ±0.051 | 85 | 1.9 ±0.32 | 0.01–0.02 | 1.4 | 11 |
3-F1TyrOMe | 6.744 ±0.021 | 160 | 2.3 ±0.17 | 0.01–0.27 | 2.7 | 13 |
3,5-F2TyrOMe | 6.802 ±0.33 | 160 | 2.7 ±0.43 | 0.01–0.12 | 2.5 | 11 |
4-BrPhe | 7.375 ±0.075 | 38 | 1.6 ±0.26 | 0.02–0.13 | 0.6 | 10 |
TrpD | ||||||
Trp | 7.045 ±0.034 | 90 | 1.8 ±0.22 | 0.01–0.15 | 1.4 | 13 |
F3Trp | 8.037 ±0.017 | 9.2 | 3.1 ±0.39 | 0.53–9.5 | 0.15 | 12 |
Ser172 | ||||||
Thr | 7.247 ±0.034 | 57 | 1.8 ±0.21 | 1.2–44 | 1 | 11 |
Tah | 6.299 ±0.028 | 500 | 2.6 ±0.31 | 0.66–41 | 7.6 | 16 |
Leu 114 | ||||||
Leu | 7.108 ±0.042 | 78 | 2.9 ±0.2 | 0.04–12 | 1.3 | 18 |
Lah | 7.056 ±0.028 | 88 | 1.6 ±0.024 | 0.01–0.60 | 1.4 | 8 |
NS6740, 1,4-diazabicyclo[3.2.2]nonan-4-yl(5-(3-(trifluoromethyl)phenyl)furan-2-yl)methanone; PNU-120596, 1-(5-chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl)-urea; WT, wild type.