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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 treatment of Alzheimer’s disease are discussed.
Kenneth J. Broadley, David R. Kelly
doaj +7 more sources
Long-Acting Muscarinic Antagonists Under Investigational to Treat Chronic Obstructive Pulmonary Disease. [PDF]
J Exp Pharmacol, 2020 Introduction Bronchodilators are the cornerstone of chronic obstructive pulmonary disease (COPD) therapy and long-acting muscarinic antagonists (LAMAs) as a mono or combination treatment play a pivotal role.
Ora J +4 more
europepmc +4 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 +6 more sources
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.
europepmc +4 more sources
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
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
openalex +4 more sources
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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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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Emerging role of long acting muscarinic antagonists for asthma. [PDF]
Br J Clin Pharmacol, 2014 Lipworth BJ.
europepmc +2 more sources