Table 1

Affinity profiles of selective and nonselective muscarinic receptor antagonists for muscarinic M2 and M3 receptors.


M2*
M3#


4-DAMP
7.8
9.0
[8, 11]
AQ-RA 741
8.3
7.5–6.6
[135]
Gallamine
6.5
4.3
[8]
DAU 5884
6.6
8.7
[14]
Methoctramine
7.5
6.5
[8]
Pirenzepine
6.2
6.8
[8, 11]
AF-DX 116
7.0
5.6–6.3
[8, 11]
Ipratropium
9.7
9.7
[5]

Tiotropium
10.7
11.0
[5]

* Data represent binding affinities (pKi) for cardiac muscarinic M2 receptors

# Data represent functional affinities (pA2) to methacholine-induced contraction of tracheal and bronchial preparations.

† Data represent binding affinities (pKi) to cloned human muscarinic receptor subtypes.

Gosens et al. Respiratory Research 2006 7:73   doi:10.1186/1465-9921-7-73

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