Results 191 to 200 of about 13,157 (218)

Bronchodilation of umeclidinium, a new long-acting muscarinic antagonist, in COPD patients

Respiratory Physiology and Neurobiology, 2013
This 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 ...
Gregory Feldman, Jean Brooks, Rashmi Mehta   +2 more
exaly   +3 more sources

Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists

Journal of Medicinal Chemistry, 2008
High 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, Yonghui, Wang, Dongchuan, Shi, Feng, Wang, Roderick S, Davis, Qi, Jin, Wei, Fu, James J, Foley, Edward F, Webb, Chris J, Dehaas, Manuela, Berlanga, Miriam, Burman, Henry M, Sarau, Dwight M, Morrow, Parvathi, Rao, Lorena A, Kallal, Michael L, Moore, Ralph A, Rivero, Michael, Palovich, Michael, Salmon, Kristen E, Belmonte, Jakob, Busch-Petersen   +21 more
openaire   +2 more sources

Long-acting muscarinic receptor antagonists for the treatment of respiratory disease

Pulmonary Pharmacology & Therapeutics, 2013
The 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, Page C, MATERA, Maria Gabriella   +2 more
openaire   +4 more sources

Long-acting muscarinic antagonists

Expert Review of Clinical Pharmacology, 2015
Chronic 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.
openaire   +2 more sources

Long-acting formulation of a new muscarinic receptor antagonist for the treatment of overactive bladder

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, Chaojun, Jiang, Fengying, Sun, Chunmei, Li, Lirong, Teng, Qingfan, Meng, Robert J, Lee, Youxin, Li   +7 more
openaire   +2 more sources

Long-acting muscarinic antagonists for the treatment of chronic obstructive pulmonary disease

Expert Review of Clinical Pharmacology, 2010
Muscarinic 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

Comparison of the in vitro pharmacological profiles of long-acting muscarinic antagonists in human bronchus

Pulmonary Pharmacology & Therapeutics, 2018
Long-acting muscarinic antagonists (LAMAs) have been recommended for the treatment of chronic obstructive pulmonary disease and (more recently) asthma. However, the in vitro pharmacological profiles of the four LAMAs currently marketed (tiotropium, umeclidinium, aclidinium and glycopyrronium) have not yet been compared (relative to ipratropium) by ...
Naline, Emmanuel, Grassin Delyle, Stanislas, Salvator, Hélène, Brollo, Marion, Faisy, Christophe, Victoni, Tatiana, Abrial, Charlotte, Devillier, Philippe   +7 more
openaire   +4 more sources

Preclinical Evaluation of Long-Acting Muscarinic Antagonists: Comparison of Tiotropium and Investigational Drugs

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, Thierry, Bouyssou, Sabine, Germeyer, Andreas, Schnapp, Florian, Gantner, Michael, Pieper   +5 more
openaire   +2 more sources

Discovery of Biphenyl Piperazines as Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists

Journal of Medicinal Chemistry, 2008
A series of novel biphenyl piperazines was discovered as highly potent muscarinic acetylcholine receptor antagonists via high throughput screening and subsequent optimization. Compound 5c with respective 500- and 20-fold subtype selectivity for M3 over M2 and M1 exhibited excellent inhibitory activity and long duration of action in a ...
Jian, Jin, Brian, Budzik, Yonghui, Wang, Dongchuan, Shi, Feng, Wang, Haibo, Xie, Zehong, Wan, Chongye, Zhu, James J, Foley, Edward F, Webb, Manuela, Berlanga, Miriam, Burman, Henry M, Sarau, Dwight M, Morrow, Michael L, Moore, Ralph A, Rivero, Michael, Palovich, Michael, Salmon, Kristen E, Belmonte, Dramane I, Lainé   +19 more
openaire   +2 more sources

Long-acting muscarinic M3 receptor antagonists.

Expert opinion on therapeutic patents, 2010
A series of 10 closely related patent applications define Theravance's approach to the development of long-acting M(3) selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore attached to a second, less ...
openaire   +2 more sources