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Table 1 Affinity profiles of selective and nonselective muscarinic receptor antagonists for muscarinic M2 and M3 receptors.

From: Muscarinic receptor signaling in the pathophysiology of asthma and COPD

 

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]

  1. * Data represent binding affinities (pKi) for cardiac muscarinic M2 receptors
  2. # Data represent functional affinities (pA2) to methacholine-induced contraction of tracheal and bronchial preparations.
  3. † Data represent binding affinities (pKi) to cloned human muscarinic receptor subtypes.