Results 1 to 10 of about 22,381 (161)
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
europepmc +4 more sources
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
doaj +2 more sources
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
doaj +3 more sources
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
doaj +2 more sources
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.
europepmc +3 more sources
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
doaj +1 more source
Biomedicines, 2023 Psychosis that occurs over the course of Alzheimer’s disease (AD) is associated with increased caregiver burden and a more rapid cognitive and functional decline.
Heidy Jimenez +9 more
doaj +1 more source
Toxins, 2021 Arecoline is one of the nicotinic acid-based alkaloids, which is found in the betel nut. In addition to its function as a muscarinic agonist, arecoline exhibits several adverse effects, such as inducing growth retardation and causing developmental ...
Petrus Siregar +10 more
doaj +1 more source
Communications Biology, 2021 Katayama et al. report a vibrational spectroscopic study using ATR–FTIR of the human M2 muscarinic acetylcholine receptor (M2R). Their work involves an extensive comparison of agonists, antagonists, and inverse agonists, in which they show that they C ...
Kota Katayama +8 more
doaj +1 more source
Journal of Pharmacological Sciences, 2008 Lung cancer is the leading cause of cancer death worldwide and new treatment strategies are clearly needed. The recent discovery that lung and other cancers synthesize and secrete acetylcholine (ACh) which acts as an autocrine growth factor suggests that
Therapy Pingfang Song, Eliot R. Spindel
doaj +1 more source