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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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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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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Isomerization of the muscarinic receptor . antagonist complex.
Journal of Biological Chemistry, 1979 The mechanism of binding of two antagonists, 3-quinuclidinyl benzilate and N-methyl-4-piperidinyl benzilate, to the muscarinic receptor was studied. The pseudo-first order rate constant of association showed a hyperbolic dependence on the concentration of the antagonist(s) indicating that the interaction involves two equilibria.
Jaak Järv +2 more
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Molecular probes for muscarinic receptors: Functionalized congeners of selective muscarinic antagonists [PDF]
Life Sciences, 1995 The muscarinic agonist oxotremorine and the tricyclic muscarinic antagonists pirenzepine and telenzepine have been derivatized using a functionalized congener approach for the purpose of synthesizing high affinity ligand probes that are suitable for conjugation with prosthetic groups, for receptor cross-linking, fluorescent and radioactive detection ...
Kenneth A. Jacobson +2 more
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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 +5 more sources
Migrastatin Acts as a Muscarinic Acetylcholine Receptor Antagonist [PDF]
The Journal of Antibiotics, 2006 Migrastatin and its analogs have various biological activities such as inhibition of cell migration and anchorage-independent growth of cancer cells. Although its biosynthesis and chemical synthesis have been under investigation, little is known about the biological target of migrastatin.
Koichi Nakae +3 more
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Positioning of Long-Acting Muscarinic Antagonists in the Management of Asthma. [PDF]
Allergy Asthma Immunol Res, 2017 Aalbers R, Park HS.
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Association of Inhaled Corticosteroids and Long-Acting Muscarinic Antagonists With Asthma Control in Patients With Uncontrolled, Persistent Asthma: A Systematic Review and Meta-analysis. [PDF]
JAMA, 2018 Sobieraj DM +8 more
europepmc +4 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
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