Results 281 to 290 of about 43,320 (312)
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Quinuclidin-2-ene - based muscarinic antagonists
Life Sciences, 1995A series of achiral 3-heteroaryl substituted quinuclidin-2-ene derivatives and related compounds have been synthesized by facile methods. The compounds were evaluated for muscarinic and antimuscarinic properties in receptor binding studies using (-)-[3H]-QNB as the radioligand and in a functional assay using isolated guinea pig urinary bladder.
U, Hacksell +5 more
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MUSCARINIC RECEPTOR ANTAGONISTS
1991A 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, 1999Although 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 +2 more
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Long-acting muscarinic antagonists
Expert Review of Clinical Pharmacology, 2015Chronic 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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Role of muscarinic antagonists in asthma therapy
Expert Review of Respiratory Medicine, 2017Higher parasympathetic tone has been reported in asthmatics. In general, cholinergic contractile tone is increased by airway inflammation associated with asthma. Nevertheless, the role of muscarinic antagonists for the treatment of asthma has not yet been clearly defined.
CAZZOLA, MARIO +3 more
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Selective muscarinic receptor antagonists for airway diseases
Current Opinion in Pharmacology, 2001Airway 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 Antagonists for Myopia Control
1998Previous 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 +3 more
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Allosteric antagonists of the muscarinic acetylcholine receptor
Biochemical Pharmacology, 1991For 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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Aprophit: An irreversible antagonist for muscarinic receptors
Biochemical Pharmacology, 1990The 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.
A H, Newman +6 more
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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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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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