Results 171 to 180 of about 12,025 (204)
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Bronchodilation of umeclidinium, a new long-acting muscarinic antagonist, in COPD patients
Respiratory Physiology and Neurobiology, 2013This study evaluated the dose-response of the new long-acting muscarinic antagonist umeclidinium (GSK573719) in patients with COPD.This randomized, double-blind, placebo-controlled, parallel-group study evaluated three once-daily doses of umeclidinium (125, 250 and 500 μg) for 28 days in 285 patients with COPD having FEV(1) of 35-70% predicted (mean ...
Glenn D Crater +2 more
exaly +3 more sources
Bronchodilatory effects of aclidinium bromide, a long-acting muscarinic antagonist, in COPD patients [PDF]
Respiratory Medicine, 2010 Aclidinium bromide is a novel, long-acting, inhaled muscarinic antagonist bronchodilator currently in Phase III clinical development for the treatment of chronic obstructive pulmonary disease (COPD). This study evaluated the pharmacodynamics, pharmacokinetics, safety and tolerability of ascending doses of aclidinium bromide in patients with COPD.This ...
E Garcia Gil, G F Joos, R A Pauwels
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Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists
Journal of Medicinal Chemistry, 2008High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via ...
Jian, Jin +21 more
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Long-acting muscarinic receptor antagonists for the treatment of respiratory disease
Pulmonary Pharmacology & Therapeutics, 2013The use of muscarinic receptor antagonists in the treatment of chronic obstructive pulmonary disease (COPD) is well established. More recently, the potential for long-acting muscarinic receptor antagonists (LAMAs) in the treatment of asthma has also been investigated.
Cazzola M +2 more
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Long-acting muscarinic antagonists
Expert Review of Clinical Pharmacology, 2015Chronic obstructive pulmonary disease (COPD) is a major cause of death and disability worldwide. Inhaled bronchodilators are the mainstay of COPD pharmacological treatment. Long-acting muscarinic antagonists (LAMAs) are a major class of inhaled bronchodilators.
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Inhaled Long-Acting Muscarinic Antagonists in Chronic Obstructive Pulmonary Disease
Future Medicinal Chemistry, 2011In 2002, the first long-acting muscarinic antagonist, tiotropium bromide (Spiriva(®)), was launched as a once-daily bronchodilating agent for the treatment of chronic obstructive pulmonary disease. Since then, there has been intense discovery research activity in this area and, currently, several alternative inhaled long-acting muscarinic antagonists ...
Jakob, Busch-Petersen, Dramane I, Lainé
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Potential for long-acting muscarinic antagonists in chronic obstructive pulmonary disease
Expert Opinion on Investigational Drugs, 2010The prevention and relief of symptoms by regular use of bronchodilators is central to the pharmacological management of chronic obstructive pulmonary disease (COPD).The aim of this article is to review the effects of inhaled muscarinic antagonists in the treatment of stable COPD.An update of the clinical studies performed with the long-acting inhaled ...
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Journal of Microencapsulation, 2012
A new muscarinic receptor antagonist, 5-hydroxymethyl tolterodine (5-HMT), was successfully encapsulated into PLGA microspheres. With an increase of PLGA concentration from 15% to 40%, encapsulation efficiency of 5-HMT increased from 55.39% to 76.32%, and the particle size of microsphere increased from 34.33 to 70.48 µm.
Lesheng, Teng +7 more
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A new muscarinic receptor antagonist, 5-hydroxymethyl tolterodine (5-HMT), was successfully encapsulated into PLGA microspheres. With an increase of PLGA concentration from 15% to 40%, encapsulation efficiency of 5-HMT increased from 55.39% to 76.32%, and the particle size of microsphere increased from 34.33 to 70.48 µm.
Lesheng, Teng +7 more
openaire +2 more sources
The Journal of Pharmacology and Experimental Therapeutics, 2009
Chronic obstructive pulmonary disease (COPD) is characterized by progressive airflow limitation caused by persistent inflammatory processes in the airways. An increased cholinergic tone mediates different pathophysiological features of COPD, such as bronchoconstriction and mucus hypersecretion, mostly through activation of the human muscarinic M(3 ...
Paola, Casarosa +5 more
openaire +2 more sources
Chronic obstructive pulmonary disease (COPD) is characterized by progressive airflow limitation caused by persistent inflammatory processes in the airways. An increased cholinergic tone mediates different pathophysiological features of COPD, such as bronchoconstriction and mucus hypersecretion, mostly through activation of the human muscarinic M(3 ...
Paola, Casarosa +5 more
openaire +2 more sources
Long-acting muscarinic antagonists for the treatment of chronic obstructive pulmonary disease
Expert Review of Clinical Pharmacology, 2010Muscarinic acetylcholine receptor antagonists, particularly of the M(3) subtype, are useful therapeutics as bronchodilators in chronic obstructive pulmonary disease (COPD). The first long-acting muscarinic antagonist, tiotropium bromide (Spiriva(®)), was launched in 2002 and has since become established as the gold-standard muscarinic antagonist for ...
openaire +2 more sources