The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT 3 receptors

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The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT3 receptors

Scopolamine is a high affinity muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. 5-HT3 receptor antagonists are used for the same purpose and are structurally related to scopolamine. To examine whether 5-HT3 receptors are affected by scopolamine we examined the effects of this drug on the electrophysiological and ligand binding properties of 5-HT3A rec...

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How can 5-HT(3) receptor antagonists exert analgesic properties?

See "Ondansetron pretreatment reduces pain on injection of propofol" by Zahedi H, Maleki A, Rostami G on pages 239-243 (1). 5-HT3 receptors occur on various components of the pain modulation system. Expressed on peripheral nerve endings and autonomic afferents as well as in the monoaminergic descending inhibitory system and certain brain regions, 5-HT3 receptors play an indispensable role in sp...

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[Selective muscarinic receptor antagonists].

3ubtypes of muscarmic receptors, first hypothesized by Birdsall et al. ~ to explain the anomalous binding of cholinergic agonists to brain receptors~ were later demonstrated with the seEective muscarinic antagonist, pirenzepine 2. Interestingly, the search for selective antagonists, which usually follows the acceptance of a concept, antedated by many years the notion of heterogeneity of rmecari...

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Muscarinic Receptor Agonists and Antagonists

A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed. A selection of chemical routes are described, which illustrate contemporary methodology for the synthes...

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ژورنال

عنوان ژورنال: Neuropharmacology

سال: 2016

ISSN: 0028-3908

DOI: 10.1016/j.neuropharm.2016.04.027