Results 241 to 250 of about 578,217 (295)

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.
N H, Lee, E E, el-Fakahany
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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
N J, Birdsall, A S, Burgen, C R, Hiley, E C, Hulme   +3 more
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MUSCARINIC RECEPTOR ANTAGONISTS

1991
A muscarinic receptor antagonist of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is N or (a) where R is H, halo or C1-C4 alkyl; R is H or C1-C4 alkyl; R is H or C1-C4 alkyl; Y is a direct link, O or S; m is an integer of from 1 to 4; n is 2 or 3; and R is 1- or 2-naphthyl or a group of formula (b), (c) or Het where R and R are ...
PFIZER LTD, PFIZER
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Muscarinic receptor agonists and antagonists

Expert Opinion on Therapeutic Patents, 1999
Although four different subtypes of the muscarinic acetylcholine (ACh) receptor with functional correlates are known to exist (function for M5 is still unclear), all muscarinic agonists and antagon...
Darius P Zlotos, Wiebke Bender, Ulrike Holzgrabe   +2 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
K, Gulya, D, Budai, P, Kása
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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
W, Greenlee, J, Clader, T, Asberom, S, McCombie, J, Ford, H, Guzik, J, Kozlowski, S, Li, C, Liu, D, Lowe, S, Vice, H, Zhao, G, Zhou, W, Billard, H, Binch, R, Crosby, R, Duffy, J, Lachowicz, V, Coffin, R, Watkins, V, Ruperto, C, Strader, L, Taylor, K, Cox   +23 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.
Sek-Jin Chew, Sek-Tien Hoh, Jenny Tan, Hong-Ming Cheng   +3 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.
A M, Lee, D B, Jacoby, A D, Fryer
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MUSCARINIC RECEPTOR ANTAGONISTS IN THE TREATMENT OF OVERACTIVE BLADDER

BJU International, 2000
ABSTRACT A wealth of clinical evidence supports the view that muscarinic receptor antagonists are effective in the treatment of overactive bladder. However, treatment‐limiting adverse effects such as dry mouth, constipation, and blurred vision have restricted the usefulness of previously available agents, such as ...
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Role of muscarinic receptor antagonists in urgency and nocturia

BJU International, 2005
The overactive bladder (OAB) syndrome is defined as urgency, with or without urgency incontinence, usually accompanied by frequency and nocturia. Muscarinic receptor antagonists are the most established form of treatment for OAB, but until recently their effectiveness was only confirmed for symptoms of incontinence and frequency.
Martin C, Michel, Jean J M C H, de la Rosette   +1 more
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