PMID: 7522861Jul 1, 1994Paper

The effect of allosteric antagonists in modulating muscarinic M2-receptor function in guinea-pig isolated trachea

British Journal of Pharmacology
D SpinaC P Page

Abstract

1. We have assessed the influence of a range of synthetic cationic polypeptides with putative inhibitory actions at prejunctional muscarinic M2-receptors on electrical field stimulation-induced contraction of guinea-pig isolated tracheal preparations. Electrical field stimulation of epithelium-denuded guinea-pig trachea resulted in frequency-dependent contractile responses. As expected, tracheal smooth muscle sensitivity to electrical field stimulation was increased in tissues pretreated with the muscarinic M2-receptor antagonist, gallamine. In contrast, gallamine did not significantly alter the contractile potency to acetylcholine. 2. Unlike gallamine, the synthetic cationic polypeptides, poly-L-arginine, poly-L-lysine, poly-D-lysine, the cationic dye ruthenium red and the anionic polysaccharide, heparin, failed to increase significantly tracheal smooth muscle sensitivity to electrical field stimulation. 3. Poly-L-arginine, ruthenium red and heparin had no effect on the contractile response to exogenously applied methacholine. 4. These data are consistent with the concept that in guinea-pig tracheal smooth muscle, gallamine is an allosteric antagonist of guinea-pig tracheal muscarinic M2-receptors, whereas the various cationic...Continue Reading

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Citations

Apr 27, 2000·American Journal of Respiratory Cell and Molecular Biology·J Mark Madison, C M Schramm
Jul 13, 2001·Pulmonary Pharmacology & Therapeutics·R Lever, C Page
Sep 2, 2003·American Journal of Physiology. Lung Cellular and Molecular Physiology·Deborah A SawatzkyRichard W Costello

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