Results 221 to 230 of about 50,615 (267)
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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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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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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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Affinitu profile of the novel muscarinic antagonist guanylpirenzepine
Life Sciences, 1990The study reports the functional affinity of an amidino derivative of pirenzepine, guanylpirenzepine, for muscarinic receptors mediating relaxation of rat duodenum, inhibition of rabbit vas deferens twitch contraction (both receptors previously classified as M1), guinea pig negative inotropism (M2) and ileal contraction (M3).
R, Micheletti +6 more
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Muscarinic agonists and antagonists in the treatment of Alzheimer's disease
Il Farmaco, 2001Alzheimer'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 +23 more
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MUSCARINIC RECEPTOR ANTAGONISTS IN THE TREATMENT OF OVERACTIVE BLADDER
BJU International, 2000ABSTRACT 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, 2005The 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 +1 more
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A study of muscarinic receptor heterogeneity with weak antagonists
European Journal of Pharmacology, 1976A study of heterogeneity among muscarinic receptors was carried out with new rigid molecules, comprising structures in the fused quinuclidine-valerolactone, quinuclidine-cyclohexenone, quinuclidine-cyclohexanone and quinuclidine-cyclohexane derivatives.
A, Fisher +4 more
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Identification and characterization of m4 selective muscarinic antagonists
Bioorganic & Medicinal Chemistry Letters, 1997Our interest in the area of m4 muscarinic antagonists had led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7 nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors.
C E, Augelli-Szafran +5 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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