Results 231 to 240 of about 556,376 (281)

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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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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Muscarinic Antagonists for Myopia Control

1998
Previous nonsurgical treatment of myopia using optical and pharmaceutical agents has not allowed an unequivocal consensus. Such studies must be based on the natural history of myopia progression, accurate biometric measurements, and randomized clinical trials.
Hong-Ming Cheng, Hong-Ming Cheng, Sek-Jin Chew, Sek-Tien Hoh, Jenny Tan   +4 more
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Muscarinic autoreceptors are differentially affected by selective muscarinic antagonists in rat hippocampus

Neurochemistry International, 1989
The effects of atropine, pirenzepine and AF-DX 116 on the high K(+)-evoked release of endogenous ACh from rat hippocampal slices were compared. As expected, atropine in concentrations of 10(?5) and 10(?6)M increased the release of acetylcholine, to 128 and 157% of the control value, respectively. While AF-DX 116 was also able to increase the release to
Dénes Budai, Peter Kasa, Karoly Gulya
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Improved Muscarinic Antagonists as Anticholinesterase Antidotes [PDF]

, 1990
Abstract : Muscarinic antagonists play an important role in anticholinesterase agent therapy by reducing the response of muscarinic receptors to acetylcholine, acting synergistically with cholinesterase reactivators. Therapy with antagonists such as atropine is difficult to manage because of the toxicity of these compounds, atropine antagonizes the ...
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Muscarinic agonists and antagonists in the treatment of Alzheimer's disease

Il Farmaco, 2001
Alzheimer's disease (AD) is a neurodegenerative disease characterized by cognitive impairment and personality changes. The development of drugs for the treatment of the cognitive deficits of AD has focused on agents which counteract loss in cholinergic activity. Although symptoms of AD have been successfully treated with acetylcholinesterase inhibitors
Vicki L. Coffin, Stuart W. McCombie, William Billard, Robert W. Watkins, Joseph A. Kozlowski, William J. Greenlee, C Liu, Jean E. Lachowicz, Lisa A. Taylor, Vilma Ruperto, Catherine D. Strader, Henry Guzik, Vice Susan F, Herbert Binch, Shengjian Li, Ruth A. Duffy, Derek B. Lowe, H Zhao, Kathleen Cox, Theodros Asberom, R Crosby, Gouwei Zhou, Jennifer Ford, John W. Clader   +23 more
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Selective muscarinic receptor antagonists for airway diseases

Current Opinion in Pharmacology, 2001
Airway tone and airway hyperreactivity are mediated by the parasympathetic nerves that release acetylcholine onto muscarinic receptors (M1-M5). Stimulation of M1 and M3 muscarinic receptors causes bronchoconstriction. The M1 muscarinic receptor is excitatory, and facilitates neuronal transmission at the parasympathetic ganglion.
David B. Jacoby, Ann M. Lee, Allison D. Fryer   +2 more
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