Selective muscarinic antagonists as bronchodilators.
The non-selective muscarinic antagonist ipratropium is widely used as bronchodilator. Due to its pharmacokinetic properties this drug, after inhalation, acts only locally on the airways and no unwanted anticholinergic side-effects are observed. Another approach is the use of selective muscarinic antagonists. Based on their selectivity for M3- and/or M1-receptors such drugs might show bronchospasmolytic properties without the occurrence of typical atropine-like side effects even after systemic administration. Pharmacological data of the in vivo bronchoselectivity of pirenzepine (M1-selective) and AQ-RA 721 (high affinity for M1- and M3-receptors) is presented and the use of these drugs as bronchodilators is discussed.
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Division of Pharma Research, Dr. Karl Thomae GmbH, Biberach, FRG.
D000818:Animals; D001993:Bronchodilator Agents / Q000494:pharmacology*; D006801:Humans; D009116:Muscarine / Q000037:antagonists & inhibitors*; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D011976:Receptors, Muscarinic / Q000378:metabolism; D012137:Respiratory System / Q000378:metabolism; D012472:Salivation / Q000187:drug effects
D001993:Bronchodilator Agents; D011976:Receptors, Muscarinic; C073026:AQ-RA 721; D010890:Pirenzepine; D009116:Muscarine