Alcuronium concentrations (−log values) for half maximum effects as estimates of the alcuronium binding affinity under the indicated assay conditions.
| Assay | Alcuronium Concentrations (−log values) for Half-Maximal Effects | Reference | ||
|---|---|---|---|---|
| Free M2Receptors | Pilocarpine Occupied M2 Receptors | Oxotremorine M Occupied M2 Receptors | ||
| Contraction force of guinea pig left atria | 5.54 (shift of oxotremorine M curve, Fig.2B) | 5.63 (reduction of pilocarpineE max, Fig.1B) | No evidence for ternary complex formation up to 100 μM alcuronium | This study |
| [35S]GTPγS binding in M2 expressing CHO cells | 5.86 (inverse agonist action, Fig.4B) | 5.47 (reduction of pilocarpine E max, Fig.4B) | No evidence for ternary complex formation up to 1000 μM alcuronium | This study |
| 5.97 (shift of oxotremorine M curve, Fig.5B) | ||||
| Radioligand binding in M2 containing membranes | 6.142-a | 6.572-a | No evidence for ternary complex formation2-a | Jakubı́k et al., 1997 2-a |
| 6.09 (Fig.6B) | 6.04 (Fig.6B) | 4.28 (Fig.6B) | This study | |
↵2-a Radioligand binding data taken from Jakubik et al. (1997) (membranes of CHO cells expressing human M2receptors; 136 mM NaCl, 5 mM KCl, 1 mM MgSO4, 1 mM sodium phosphate buffer, 0.5 mM GTP, 10 mM sodium HEPES, pH 7.4, 25°C).