Table 1.
Properties of wildtype and mutant P2X1Rs that showed a change in MTSEA-biotinylation in response to PPADS treatment
Peak currents to a maximal concentration of ATP and the sensitivity to ATP (pEC50), the EC90 concentration used for determination of antagonist sensitivity and PPADS (pIC50); data are shown as mean ± S.D.
| Mutants | Peak | n | pEC50 | EC50 | n | EC90 | pIC50 | IC50 | n |
|---|---|---|---|---|---|---|---|---|---|
| μA | μm | μm | μm | ||||||
| WT | −10.06 ± 3.58 | 37 | 6.12 ± 0.16 | 0.8 | 4 | 10 | 6.12 ± 0.15 | 0.8 | 5 |
| S64C | −13.47 ± 0.96 | 5 | 5.90 ± 0.11 | 1.2 | 3 | 10 | 6.12 ± 0.25 | 0.8 | 4 |
| S66C | −11.56 ± 0.73 | 4 | 5.80 ± 0.11 | 1.6 | 3 | 10 | 6.14 ± 0.33 | 0.7 | 3 |
| K70C | −4.21 ± 0.88a | 3 | 4.34 ± 0.16b | 45.9 | 3 | 300 | 5.64 ± 0.10a | 2.3 | 3 |
| V74C | −10.46 ± 0.81 | 6 | 6.02 ± 0.10 | 1.0 | 3 | 10 | 6.10 ± 0.02 | 0.8 | 4 |
| T75C | −7.60 ± 2.57 | 4 | 5.60 ± 0.05c | 2.5 | 3 | 10 | 5.82 ± 0.25 | 1.5 | 3 |
| L77C | −11.23 ± 2.34 | 6 | 5.93 ± 0.09 | 1.2 | 3 | 10 | 5.90 ± 0.28 | 1.3 | 4 |
| G123C | −6.61 ± 4.63 | 6 | 5.21 ± 0.07b | 6.1 | 4 | 30 | 5.79 ± 0.18 | 1.6 | 6 |
| K138C | −14.47 ± 2.42a | 5 | 6.34 ± 0.09 | 0.5 | 3 | 10 | 5.56 ± 0.31b | 2.8 | 5 |
| R139C | −16.96 ± 1.16b | 5 | 6.22 ± 0.07 | 0.6 | 3 | 10 | 5.78 ± 0.14 | 1.7 | 6 |
| D170C | −10.90 ± 0.2 | 5 | 5.69 ± 0.14c | 2.1 | 5 | 10 | 6.62 ± 0.19d | 0.2 | 8 |
| A182C | −7.24 ± 2.11 | 4 | 6.26 ± 0.25 | 0.6 | 3 | 10 | 6.32 ± 0.11 | 0.5 | 4 |
| K190C | −5.39 ± 0.49a | 4 | 5.46 ± 0.06b | 3.5 | 3 | 30 | 5.54 ± 0.22c | 2.9 | 3 |
| E248C | −12.76 ± 3.20 | 4 | 6.70 ± 0.24d | 0.2 | 3 | 10 | 5.88 ± 0.24 | 1.3 | 4 |
| K249C | −11.87 ± 1.86 | 4 | 6.10 ± 0.17 | 0.7 | 6 | 10 | 5.60 ± 0.13d | 2.5 | 7 |
| L279C | −12.59 ± 1.87 | 8 | 6.30 ± 0.20 | 0.5 | 3 | 10 | 5.98 ± 0.36 | 1.1 | 5 |
| N284C | −11.95 ± 4.19 | 7 | 5.64 ± 0.06a | 2.3 | 3 | 10 | 6.34 ± 0.13 | 0.5 | 5 |
a p < 0.05.
b p < 0.0001.
c p < 0.01.
d p < 0.001.