The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT3 receptors. [PDF]
Neuropharmacology, 2016 Scopolamine is a high affinity muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. 5-HT3 receptor antagonists are used for the same purpose and are structurally related to scopolamine. To examine whether 5-HT3 receptors are affected by scopolamine we examined the effects of this drug on the electrophysiological ...
Lochner M, Thompson AJ.
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Long-Acting Muscarinic Antagonists Under Investigational to Treat Chronic Obstructive Pulmonary Disease [PDF]
Journal of Experimental Pharmacology, 2020 Josuel Ora,1 Angelo Coppola,2 Mario Cazzola,3 Luigino Calzetta,4 Paola Rogliani1,3 1Division of Respiratory Medicine, University Hospital Tor Vergata, Rome, Italy; 2Division of Respiratory Medicine, San Filippo Neri Hospital, Rome, Italy; 3Department of ...
Ora J +4 more
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Investigating the Unbinding of Muscarinic Antagonists from the Muscarinic 3 Receptor. [PDF]
J Chem Theory Comput, 2023 Patient symptom relief is often heavily influenced by the residence time of the inhibitor-target complex. For the human muscarinic receptor 3 (hMR3), tiotropium is a long-acting bronchodilator used in conditions such as asthma or chronic obstructive pulmonary disease (COPD). The mechanistic insights into this inhibitor remain unclear; specifically, the
Buigues PJ +7 more
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Muscarinic Receptor Agonists and Antagonists [PDF]
Molecules, 2001 A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the ...
David R. Kelly, Kenneth J. Broadley
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The Impact of Muscarinic Receptor Antagonists on Airway Inflammation: A Systematic Review
International Journal of COPD, 2021 Luigino Calzetta,1 Angelo Coppola,2 Beatrice Ludovica Ritondo,3 Matteo Matino,3 Alfredo Chetta,1 Paola Rogliani2,3 1Department of Medicine and Surgery, Respiratory Disease and Lung Function Unit, University of Parma, Parma, Italy; 2Division of ...
Calzetta L +5 more
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Positioning of Long-Acting Muscarinic Antagonists in the Management of Asthma. [PDF]
Allergy Asthma Immunol Res, 2017 Despite a range of efficacious therapies for asthma, including inhaled corticosteroids (ICS) and long-acting β2-agonists (LABA), a significant proportion of patients have poor asthma control and retain a risk of future worsening of their symptoms.
Aalbers R, Park HS.
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Multitargeting nature of muscarinic orthosteric agonists and antagonists
Frontiers in Physiology, 2022 Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
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Emerging role of long acting muscarinic antagonists for asthma. [PDF]
Br J Clin Pharmacol, 2014 Lipworth BJ.
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Efficacy and Safety of DA-8010, a Novel M3 Antagonist, in Patients With Overactive Bladder: A Randomized, Double-Blind Phase 2 Study [PDF]
International Neurourology Journal, 2022 Purpose DA-8010 is a novel muscarinic M3 receptor antagonist with significant selectivity for bladder over salivary gland in preclinical studies. We evaluated the clinical efficacy and safety of DA-8010 in overactive bladder (OAB) patients.
Hee Seo Son +12 more
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