Abstract
Synthesis and biological activity of a novel class of quaternary ammonium salt muscarinic M3 receptor antagonists, showing high selectivity versus the M2 receptor, are described. Selected compounds exhibited potent anticholinergic properties, in isolated guinea-pig trachea, and good functional selectivity for trachea over atria. In vivo, the same compounds potently inhibited acetylcholine-induced bronchoconstriction after intratracheal administration in the guinea pig.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Bronchoconstriction / drug effects
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Bronchodilator Agents / chemical synthesis
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Bronchodilator Agents / chemistry*
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Bronchodilator Agents / pharmacology
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CHO Cells
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Cricetinae
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Cricetulus
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Guinea Pigs
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Humans
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Imidazolidines / chemical synthesis*
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Imidazolidines / chemistry
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Imidazolidines / pharmacology
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In Vitro Techniques
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Male
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Muscle, Smooth / physiology
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Myocardial Contraction / drug effects
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Quaternary Ammonium Compounds / chemical synthesis*
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Quaternary Ammonium Compounds / chemistry
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Quaternary Ammonium Compounds / pharmacology
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Radioligand Assay
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Receptor, Muscarinic M3 / antagonists & inhibitors*
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Structure-Activity Relationship
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Trachea / drug effects
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Trachea / physiology
Substances
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Bronchodilator Agents
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Imidazolidines
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Quaternary Ammonium Compounds
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Receptor, Muscarinic M3