TABLE 2

Parameters characterizing the interaction of orthosteric ligands with the equilibrium binding of [3H]dimethyl-W84 and [3H]NMS at M2 receptors

The data are mean values ± S.E.M. of three to seven independent experiments. For details see text.

[3H]dimethyl-W84 [3H]NMS logKX,orthoster - logKi,orthoster
Orthosteric agent logKX,orthoster α logKi,orthosternH
(+)-Dexetimide 9.03±0.07 0.02±0.03 8.93±0.19 1.07±0.08 0.10
NMS 9.40±0.12 0.19±0.03 9.37±0.16a 1.01±0.05 0.03
(-)-Scopolamine 8.63±0.12 0.08±0.01 8.59±0.19 1.01±0.08 0.04
Atropine 8.36±0.07 0.20±0.02 8.66±0.20 1.01±0.08 -0.30
AF-DX 384 8.03±0.06 0.09±0.02 8.09±0.26 0.96±0.13 -0.06
NBS 6.77±0.07 0.07±0.02 6.78±0.20 1.04±0.08 -0.01
(-)-Levetimide 5.18±0.04b b 5.32±0.17 1.02±0.08 N.D.
  • N.D., not determined

  • a Value is the log affinity constant of [3H]NMS

  • b The log affinity constant derived from logistic curve fitting