TABLE 1

Parameters characterizing the interactions of allosteric agents with the equilibrium binding of [3H]dimethyl-W84 and with the equilibrium binding and dissociation of [3H]NMS from M2 receptors

The data are mean values ± S.E.M. of 3 to 22 experiments carried out in triplicate. For details, see text.

[3H]Dimethyl-W84 [3H]NMS
Allosteric Agent logKi,allosternH logKX,alloster α log(α × KX,alloster) Measured logKX,dissnH logKi,alloster - logKX,alloster
Dimethyl-W84 8.47±0.04a 0.97±0.15 8.55±0.05 0.27±0.01 7.98 7.96±0.07 0.96±0.16 -0.08
W84 7.59±0.05 1.08±0.16 7.50±0.10 0.50±0.02 7.20 7.43±0.04 0.95±0.10 0.09
Gallamine 7.63±0.07 0.84±0.11 7.84±0.02 0.04±0.01 6.47 6.25±0.05 0.81±0.08 -0.21
WDuo3 6.91±0.04 1.06±0.05 6.60±0.18 1.5±0.1 6.78 7.29±0.11 0.92±0.25 0.31
Alcuronium 6.80±0.01 0.87±0.18 7.45±0.20 1.7±0.1 7.69 7.96±0.04 1.17±0.13 -0.65
Strychnine 5.05±0.22 0.78±0.12 N.D. N.D. N.D. N.D. N.D. N.D.
  • N.D., not determined

  • a Value is the log affinity constant, logKL, derived from homologous inhibition experiments