The 5-HT3B subunit affects high-potency inhibition of 5-HT3 receptors by morphine
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چکیده
منابع مشابه
Identification of a Domain which Affects Kinetics and Antagonistic Potency of Clozapine at 5-HT3 Receptors
The widely used atypical antipsychotic clozapine is a potent competitive antagonist at 5-HT(3) receptors which may contribute to its unique psychopharmacological profile. Clozapine binds to 5-HT(3) receptors of various species. However, the structural requirements of the respective binding site for clozapine remain to be determined. Differences in the primary sequences within the 5-HT(3A) recep...
متن کاملThe 5-HT3B subunit confers spontaneous channel opening and altered ligand properties of the 5-HT3 receptor.
Current receptor theory suggests that there is an equilibrium between the inactive (R) and active (R*) conformations of ligand-gated ion channels and G protein-coupled receptors. The actions of ligands in both receptor types could be appropriately explained by this two-state model. Ligands such as agonists and antagonists affect receptor function by stabilizing one or both conformations. The 5-...
متن کاملDeletion of the glutamate receptor 5 subunit of kainate receptors affects the development of morphine tolerance.
Previous reports utilizing pharmacological antagonists implicate kainate receptor (KAR) activation in the development of morphine tolerance, dependence, conditioned place preference (CPP), and locomotor sensitization, but the role of glutamate receptor (GluR) 5-containing KAR in these effects remains unclear because of limited selectivity of the inhibitors employed. Therefore, we examined respo...
متن کامل5-HT3 receptors and emesis
Nausea and vomiting. Nausea and vomiting is a major problem which occurs during and after the treatment with certain drugs like anesthetics, opioidanalgesics or cytostatics. Postoperative nausea and vomiting (PONV) is called the “big” little problem. As a consequence, the choice of the anesthetic drug(s) plays a role in preventing PONV [Apfel et al., Anesthesiology, 1999; Eberhart et al., Eur J...
متن کاملExpression of 5-HT3 receptors by extrinsic duodenal afferents contribute to intestinal inhibition of gastric emptying.
Intestinal perfusion with carbohydrates inhibits gastric emptying via vagal and spinal capsaicin-sensitive afferent pathways. The aim of the present study was to determine the role of 1) 5-hydroxytryptamine (5-HT)(3) receptors (5-HT(3)R) in mediating glucose-induced inhibition of gastric emptying and 2) 5-HT(3)R expression in vagal and spinal afferents in innervating the duodenum. In awake rats...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2012
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.2011.01582.x