ipratropium-bromide-anhydrous and Bronchial-Spasm

ipratropium-bromide-anhydrous has been researched along with Bronchial-Spasm* in 1 studies

Other Studies

1 other study(ies) available for ipratropium-bromide-anhydrous and Bronchial-Spasm

ArticleYear
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)ace
    Journal of medicinal chemistry, 2009, Aug-27, Volume: 52, Issue:16

    The objective of this work was to discover a novel, long-acting muscarinic M(3) antagonist for the inhaled treatment of chronic obstructive pulmonary disease (COPD), with a potentially improved risk-benefit profile compared with current antimuscarinic agents. A series of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters were synthesized and evaluated. On the basis of its overall profile, (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) emerged as a candidate for once-daily maintenance treatment of COPD. This compound is a potent muscarinic antagonist, with long duration of action in vivo, and was found to have a rapid hydrolysis in human plasma, minimizing the potential to induce class-related systemic side effects. Aclidinium bromide is currently in phase III development for maintenance treatment of patients with COPD.

    Topics: Administration, Inhalation; Animals; Bronchial Spasm; CHO Cells; Cricetinae; Cricetulus; Drug Stability; Esters; Guinea Pigs; Humans; Male; Mice; Muscarinic Antagonists; Pulmonary Disease, Chronic Obstructive; Quaternary Ammonium Compounds; Quinuclidines; Radioligand Assay; Receptor, Muscarinic M3; Stereoisomerism; Structure-Activity Relationship; Tropanes

2009