Muscarinic M3 receptors mediate contraction of human central and peripheral airway smooth muscle

✍ Scribed by A.F. Roffel; C.R.S. Elzinga; J. Zaagsma

• Publisher: Elsevier
• Year: 1990
• Tongue: English
• Weight: 469 KB
• Volume: 3
• Category: Article
• ISSN: 0952-0600
• DOI: 10.1016/0952-0600(90)90009-8

✦ Synopsis

The muscarinic receptor subtype involved in human airway smooth muscle contraction was characterised for the first time, using subtype-selective muscarinic antagonists. It was demonstrated that methacholine-induced contraction of central (trachea) and peripheral (small bronchi) airway smooth muscle preparations was antagonised by pirenzepine, AF-DX 116, 4-DAMP methobromide, hexahydrosiladifenidol, and methoctramine with pA2-values characteristic of M3 (smooth muscle/glandular) muscarinic receptors. Since these pA2-values demonstrate significant correlations with those found in bovine and guinea-pig tracheal smooth muscle contraction, it is concluded that these animal tissues provide a good model for the study of M3 subtype-selective muscarinic antagonists to be used as bronchodilators.