Results 271 to 280 of about 51,230 (302)

Selective Muscarinic Receptor Agonists and Antagonists

Pharmacology & Toxicology, 1996
Abstract:Muscarinic receptors are composed of a family of four subtypes each of which can be distinguished pharmacologically and structurally. The physiological role of each subtype in the central and peripheral nervous systems remains to be clarified, due, in part, to a lack of agonists and antagonists with adequate subtype selectivity.
Richard M. Eglen, Nikki Watson
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Muscarinic Receptor Antagonists

2016
Parasympathetic activity is increased in patients with chronic obstructive pulmonary disease (COPD) and asthma and appears to be the major reversible component of airway obstruction. Therefore, treatment with muscarinic receptor antagonists is an effective bronchodilator therapy in COPD and also in asthmatic patients.
Maria Gabriella Matera, Mario Cazzola
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Muscarinic receptor antagonists for overactive bladder

BJU International, 2007
From time to time we publish a full review of drugs that are available for the treatment of common conditions. In this issue, the review is written by two of the leading authorities in the world, Paul Abrams and Karl‐Erik Andersson, on the topic of overactive bladder and antimuscarinic agents.
Karl-Erik Andersson, Paul Abrams
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Design and synthesis of a fluorescent muscarinic antagonist

Bioorganic & Medicinal Chemistry Letters, 2008
The design and concise synthesis of a fluorescent tolterodine-BODIPY (boron dipyrromethene) conjugate is described which possesses potent antimuscarinic activity. This derivative illustrates proof-of-concept for the preparation of other useful fluorophoric antimuscarinic agents which have potential utility in receptor occupancy studies and high ...
Carolyn Napier, J. W. Watson, Lyn H. Jones, Sasha Sreckovic, Amy Randall, Mike Trevethick   +5 more
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Quinidine as a muscarinic antagonist: A structural approach

Journal of Pharmaceutical Sciences, 1992
The synthesis, spectroscopic characteristics, and single-crystal X-ray structural analysis of quitenidine methyl ester monohydrate, a derivative of the muscarinic antagonist quinidine, are presented. Quitenidine methyl ester monohydrate (C20H24N2O4.H2O) crystallizes in the orthorhombic space group P2(1)2(1)2(1), with a = 16.69(3) A, b = 12.46(2) A, c =
Barbara J. Oleksyn, Teodozja Lipinska, Maria Ciechanowicz‐Rutkowska, Alina Suszko-Purzycka   +3 more
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Aprophit: An irreversible antagonist for muscarinic receptors

Biochemical Pharmacology, 1990
The development of selective irreversible ligands has proven to be an invaluable technique for the isolation, purification and characterization of many receptor proteins. An isothiocyanato-derivative of the muscarinic antagonist aprophen was synthesized and evaluated as a potential irreversible ligand for muscarinic receptors.
Barrington W. Jackson, Amy Hauck Newman, Marvin A. Oleshansky, Joseph Covington, Haim Leader, Peter K. Chiang, Ben A. Weissman   +6 more
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Binding of agonists and antagonists to muscarinic receptors

Journal of Supramolecular Structure, 1976
AbstractThe binding of one irreversible and two reversible radioactive antagonists to muscarinic receptors in synaptosome preparations of rat cerebral cortex has been studied. The ligands all bind to the same receptor pool and directly and competitively yield self‐consistent binding constants closely similar to those obtained by pharmacological methods
Nigel J. M. Birdsall, Edward C. Hulme, Arnold S. V. Burgen, C. R. Hiley   +3 more
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Allosteric antagonists of the muscarinic acetylcholine receptor

Biochemical Pharmacology, 1991
For the most part, the interaction of these selective antagonists with muscarinic receptors has been interpreted in the context of simple competitive bimolecular reaction which obeys the law of mass action. In fact, the use of selective antagonists as a pharmacological tool to identify receptor types and subtypes is based on this premise.
Esam E. El-Fakahany, Norman H. Lee
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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.
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Emerging muscarinic receptor antagonists for the treatment of asthma

Expert Opinion on Emerging Drugs, 2020
The increased acetylcholine signaling in asthma pathophysiology offers the rationale for the use of LAMAs in the treatment of asthmatic patients. Tiotropium is still the only LAMA approved for use in asthma but there is a real interest in developing novel LAMAs for the treatment of asthma, or at least to extend this indication to other LAMAs already on
Maria Gabriella, Matera, Carmela, Belardo, Michele, Rinaldi, Barbara, Rinaldi, Mario, Cazzola   +4 more
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