TABLE 2

Binding affinities of different muscarinic antagonists against the five human muscarinic receptor subtypes The equilibrium dissociation constants of the different muscarinic antagonists were determined in heterologous competition experiments against [3H]NMS. The pKi values shown are the average of at least three independent experiments performed in triplicate, and the means ± S.E. associated with the measurements were 0.1 or less.




hM1

hM2

hM3

hM4

hM5
Atropine 9.77 9.47 9.68 9.97 9.50
NMS 10.31 10.25 10.32 10.42 9.59
Ipratropium 9.40 9.53 9.58 9.65 9.07
Pirenzepine 8.63 <7.0 7.03 7.91 7.32
Tiotropium 10.80 10.69 11.02 11.02 9.96
Aclidinium 10.78 10.68 10.74 10.84 10.26
Glycopyrrolate
10.09
9.67
10.04
10.26
9.74