From: Divergence of allosteric effects of rapacuronium on binding and function of muscarinic receptors
pKD | BMAX | pKD' | BMAX | pKD' | BMAX | |
---|---|---|---|---|---|---|
[3H]NMS | + 10 μM rapacuronium | + 100 μM rapacuronium | ||||
M1 | 9.60 ± 0.04 | 1.98 ± 0.20 | 9.14 ± 0.03* | 2.03 ± 0.15 | 8.73 ± 0.03* | 1.85 ± 0.17 |
M2 | 9.49 ± 0.03 | 1.56 ± 0.16 | 8.92 ± 0.04* | 1.62 ± 0.14 | 8.64 ± 0.03* | 1.66 ± 0.14 |
M3 | 9.64 ± 0.05 | 1.64 ± 0.17 | 9.44 ± 0.03* | 1.67 ± 0.14 | 8.96 ± 0.03* | 1.59 ± 0.16 |
M4 | 9.69 ± 0.04 | 1.19 ± 0.14 | 9.19 ± 0.02* | 1.17 ± 0.13 | 8.52 ± 0.06* | 1.06 ± 0.10 |
M5 | 9.59 ± 0.03 | 1.49 ± 0.16 | 9.31 ± 0.02* | 1.53 ± 0.15 | 8.46 ± 0.06* | 1.33 ± 0.13 |
[ 3 H]Ach | + 10 μM rapacuronium | + 100 μM rapacuronium | ||||
M1 | 7.58 ± 0.05 | 0.33 ± 0.05 | 7.12 ± 0.03* | 0.33 ± 0.05 | 6.43 ± 0.05* | 0.32 ± 0.05 |
M2 | 7.63 ± 0.03 | 0.80 ± 0.08 | 7.09 ± 0.05* | 0.74 ± 0.07 | 6.30 ± 0.06* | 0.77 ± 0.08 |
M3 | 7.67 ± 0.05 | 0.39 ± 0.05 | 7.43 ± 0.04* | 0.40 ± 0.04 | 6.85 ± 0.03* | 0.37 ± 0.05 |
M4 | 7.69 ± 0.04 | 0.55 ± 0.04 | 7.17 ± 0.03* | 0.54 ± 0.05 | 6.41 ± 0.05* | 0.47 ± 0.04 |
M5 | 7.68 ± 0.03 | 0.33 ± 0.06 | 7.43 ± 0.02* | 0.33 ± 0.03 | 6.64 ± 0.04* | 0.34 ± 0.06 |