Table 2

Alcuronium concentrations (−log values) for half maximum effects as estimates of the alcuronium binding affinity under the indicated assay conditions.

AssayAlcuronium Concentrations (−log values) for Half-Maximal EffectsReference
Free M2ReceptorsPilocarpine Occupied M2 ReceptorsOxotremorine M Occupied M2 Receptors
Contraction force of guinea pig left atria5.54 (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 alcuroniumThis study
[35S]GTPγS binding in M2 expressing CHO cells5.86 (inverse agonist action, Fig.4B)5.47 (reduction of pilocarpine E max, Fig.4B)No evidence for ternary complex formation up to 1000 μM alcuroniumThis study
5.97 (shift of oxotremorine M curve, Fig.5B)
Radioligand binding in M2 containing membranes6.142-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).