Potencies with which the compounds slow the rates of dissociation [3H]NMS from the various wild-type and mutant receptors
| M5 | M2 | CR3 | CR4 | CR5 | CR6 | M2423T→H | M5478 H→T | CR6 T→H | CR3 H→T | M4 | M4436S→T | M4436 S→H | |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| CARALL | 5.59 ± 0.08 | 8.00 ± 0.06 | 7.01 ± 0.07 | 5.66 ± 0.07 | 5.95 ± 0.04 | 6.91 ± 0.03 | 7.28 ± 0.10 | 6.55 ± 0.05 | 5.52 ± 0.06 | 7.84 ± 0.06 | |||
| CARPROG | 5.66 ± 0.06 | 8.15 ± 0.05 | 7.03 ± 0.05 | 5.25 ± 0.11 | 6.01 ± 0.05 | 6.77 ± 0.03 | 7.19 ± 0.09 | 6.49 ± 0.09 | 5.35 ± 0.09 | 7.75 ± 0.08 | 7.61 ± 0.02 | 7.51 ± 0.03 | 6.03 ± 0.06 |
| CARMETH | 5.17 ± 0.07 | 7.70 ± 0.03 | 6.07 ± 0.08 | 4.75 ± 0.12 | 5.16 ± 0.07 | 7.08 ± 0.06 | 6.50 ± 0.08 | 6.64 ± 0.03 | 4.70 ± 0.21 | 7.71 ± 0.03 | 7.18 ± 0.06 | 7.29 ± 0.06 | 5.24 ± 0.09 |
| W84 | 5.79 ± 0.06 | 7.62 ± 0.03 | 7.00 ± 0.07 | 5.66 ± 0.03 | 5.90 ± 0.03 | 6.43 ± 0.03 | 7.11 ± 0.03 | 6.49 ± 0.05 | 5.95 ± 0.03 | 7.47 ± 0.03 | |||
| Dimethyl-W84 | 5.71 ± 0.07 | 8.17 ± 0.03 | 7.22 ± 0.03 | 5.62 ± 0.06 | 5.93 ± 0.05 | 6.50 ± 0.04 | 7.51 ± 0.11 | 6.48 ± 0.02 | 6.07 ± 0.12 | 8.06 ± 0.18 | 7.31 ± 0.01 | 7.24 ± 0.02 | 6.68 ± 0.06 |
| Alcuronium | 5.32 ± 0.04 | 8.57 ± 0.05 | 7.47 ± 0.07 | 5.35 ± 0.12 | 5.72 ± 0.06 | 5.70 ± 0.03 | 8.00 ± 0.05 | 5.78 ± 0.10 | 5.68 ± 0.10 | 6.94 ± 0.04 |
Potencies are given as pEC50,diss, which is the negative logarithm of the concentration that reduced [3H]NMS dissociation to half of the control rate. As in Table 1, all point mutations are at the position homologous to M2 423. Indicated are mean values ± S.E. of two to four separate experiments.