TABLE 1

Comparison of the equilibrium and kinetic parameters of M3 antagonists under nonphysiological and physiological conditions

Data are presented as the mean ± S.E. from a representative of three or more experiments.

LigandNonphysiologicalPhysiological
pKikofft1/2pKikofft1/2
min1minmin1min1
Tiotropium11.10 ± 0.020.0015 ± 0.000246210.37 ± 0.040.015 ± 0.00246.2
NVA23710.30 ± 0.040.004 ± 0.0021739.59 ± 0.050.061 ± 0.00311.4
[3H]NMS10.45 ± 0.020.017 ± 0.001419.51 ± 0.050.31 ± 0.032.24