[3H]NMS | Gallamine | Alcuronium | ||||||
---|---|---|---|---|---|---|---|---|
Kd | koff | pKdiss | pKA | α | pKdiss | pKA | α | |
nM | min−1 | M | M | |||||
Wild-type M3 | 0.29 ± 0.006 | 0.05 ± 0 | 3.91 ± 0.02 | 4.7 ± 0.08 | 4.3 ± 0.6 | 3.70 ± 0.04 | 3.9 ± 0.09 | 2.6 ± 0.3 |
Wild-type M2 | 0.75 ± 0.051-150 | 0.34 ± 0.021-150 | 4.80 ± 0.191-150 | 6.4 ± 0.031-150 | 11 ± 0.41-150 | 6.90 ± 0.101-150 | 6.1 ± 0.21-150 | 0.3 ± 0.051-150 |
Modifications in o1 of M3 | ||||||||
R133G | 0.49 | 0.07 ± 0.0021-150 | 4.44 ± 0.081-150 | NM | Close to 11-159 | 3.71 ± 0.18 | 3.9 ± 0.03 | 1.8 ± 0.2 |
(0.50; 0.48) | ||||||||
Modifications in o2 of M3 | ||||||||
K213T | 0.33 | 0.05 ± 0.002 | 4.01 ± 0.01 | 4.5 ± 0.18 | 2.9 ± 0.4 | 3.79 ± 0.05 | 4.1 ± 0.08 | 1.6 ± 0.03 |
(0.32; 0.34) | ||||||||
P217D | 0.31 | 0.06 ± 0.0021-150 | 4.30 ± 0.041-150 | 4.8 ± 0.01 | 4.2 ± 1.0 | 4.03 ± 0.15 | 4.1 ± 0.05 | 2.4 ± 0.5 |
(0.31; 0.31) | ||||||||
P217D +P218E | 0.39 | 0.06 ± 0.0021-150 | 4.23 ± 0.061-150 | 4.6 ± 0.06 | 4.0 ± 0.8 | 3.95 ± 0.021-150 | 4.2 ± 0.03 | 2.1 ± 0.4 |
(0.39; 0.39) | ||||||||
o2M2 | 0.27 ± 0.03 | 0.06 ± 0.0031-150 | 4.75 ± 0.041-150 | 5.8 ± 0.051-150 | 4.8 ± 0.5 | 4.72 ± 0.011-150 | 4.8 ± 0.041-150 | 3.1 ± 0.8 |
Modifications in o3 of M3 | ||||||||
K523N | 0.65 | 0.15 ± 0.0031-150 | 4.54 ± 0.0031-150 | 6.1 ± 0.061-150 | 16.0 ± 1.91-150 | 4.69 ± 0.041-150 | 4.7 ± 0.201-150 | 1.8 ± 0.3 |
(0.65; 0.66) | ||||||||
KFN | 0.49 ± 0.11 | 0.22 ± 0.021-150 | 4.12 ± 0.071-150 | 6.4 ± 0.171-150 | 46.5 ± 12.01-150 | 4.72 ± 0.121-150 | NM | Close to 11-159 |
DSKFN | 0.74 ± 0.121-150 | 0.21 ± 0.011-150 | 4.21 ± 0.041-150 | 6.3 ± 0.111-150 | 25.1 ± 3.81-150 | 4.67 ± 0.071-150 | 4.4 ± 0.121-150 | 0.3 ± 0.031-150 |
Data are means ± S.E.M. of three to nine experiments; individual results have been shown where n < 3.