Literature DB >> 21342788

Allosteric modulation of the 5-HT(3) receptor.

Paul A Davies1.   

Abstract

5-Hydroxytryptamine type 3 (5-HT(3)) receptors are ligand-gated ion channels that play important roles in depression, anxiety, substance abuse, emesis, inflammatory pain, spinal nociception, gastrointestinal function, and cardiovascular reflexes. Probably the most studied modulators of 5-HT(3) receptors are the high affinity competitive 'setron' antagonists typified by ondansetron. However, there exists a broad range of compounds that modulate the 5-HT(3) receptor, not through the orthosteric site but by binding to allosteric sites. Most notable are therapeutic compounds ascribed to certain targets but that allosterically modulate 5-HT(3) receptors at clinically relevant concentrations.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21342788      PMCID： PMC3072441          DOI： 10.1016/j.coph.2011.01.010

Source DB:  PubMed          Journal:  Curr Opin Pharmacol        ISSN： 1471-4892            Impact factor:   5.547


  44 in total

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Authors:  M Barann; G Molderings; M Brüss; H Bönisch; B W Urban; M Göthert
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3.  A novel class of ligand-gated ion channel is activated by Zn2+.

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4.  Impact of lipid raft integrity on 5-HT3 receptor function and its modulation by antidepressants.

Authors:  Caroline Nothdurfter; Sascha Tanasic; Barbara Di Benedetto; Gerhard Rammes; Eva-Maria Wagner; Thomas Kirmeier; Vanessa Ganal; Julia S Kessler; Theo Rein; Florian Holsboer; Rainer Rupprecht
Journal:  Neuropsychopharmacology       Date:  2010-03-03       Impact factor: 7.853

5.  Subunit-dependent inhibition of human neuronal nicotinic acetylcholine receptors and other ligand-gated ion channels by dissociative anesthetics ketamine and dizocilpine.

Authors:  T Yamakura; L E Chavez-Noriega; R A Harris
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Review 6.  Emerging strategies for exploiting cannabinoid receptor agonists as medicines.

Authors:  Roger G Pertwee
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7.  Direct subunit-dependent multimodal 5-hydroxytryptamine3 receptor antagonism by methadone.

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8.  Volatile anaesthetics may be the main cause of early but not delayed postoperative vomiting: a randomized controlled trial of factorial design.

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9.  The nonpsychoactive cannabinoid cannabidiol inhibits 5-hydroxytryptamine3A receptor-mediated currents in Xenopus laevis oocytes.

Authors:  Keun-Hang Yang; Sehamuddin Galadari; Dmytro Isaev; Georg Petroianu; Toni S Shippenberg; Murat Oz
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10.  Identification of a domain which affects kinetics and antagonistic potency of clozapine at 5-HT3 receptors.

Authors:  Gerhard Rammes; Christine Hosp; Brigitte Eisensamer; Sascha Tanasic; Caroline Nothdurfter; Walter Zieglgänsberger; Rainer Rupprecht
Journal:  PLoS One       Date:  2009-08-21       Impact factor: 3.240
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  15 in total

Review 1.  From Chemotherapy-Induced Emesis to Neuroprotection: Therapeutic Opportunities for 5-HT3 Receptor Antagonists.

Authors:  Gohar Fakhfouri; Kazem Mousavizadeh; Sharam Ejtemaei Mehr; Ahmad Reza Dehpour; Mohammad Reza Zirak; Jean-Eric Ghia; Reza Rahimian
Journal:  Mol Neurobiol       Date:  2014-11-07       Impact factor: 5.590

Review 2.  Pharmacology of serotonin and female sexual behavior.

Authors:  Lynda Uphouse
Journal:  Pharmacol Biochem Behav       Date:  2013-11-15       Impact factor: 3.533

3.  5-Chloroindole: a potent allosteric modulator of the 5-HT₃ receptor.

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Journal:  Br J Pharmacol       Date:  2013-07       Impact factor: 8.739

Review 4.  Seeking structural specificity: direct modulation of pentameric ligand-gated ion channels by alcohols and general anesthetics.

Authors:  Rebecca J Howard; James R Trudell; R Adron Harris
Journal:  Pharmacol Rev       Date:  2014-02-10       Impact factor: 25.468

5.  The Role of 5-HT3 Receptors in Signaling from Taste Buds to Nerves.

Authors:  Eric D Larson; Aurelie Vandenbeuch; Anja Voigt; Wolfgang Meyerhof; Sue C Kinnamon; Thomas E Finger
Journal:  J Neurosci       Date:  2015-12-02       Impact factor: 6.167

6.  Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site.

Authors:  Sarah M Trattnig; Kasper Harpsøe; Sarah B Thygesen; Louise M Rahr; Philip K Ahring; Thomas Balle; Anders A Jensen
Journal:  J Biol Chem       Date:  2012-05-15       Impact factor: 5.157

7.  Sniffer patch laser uncaging response (SPLURgE): an assay of regional differences in allosteric receptor modulation and neurotransmitter clearance.

Authors:  Catherine A Christian; John R Huguenard
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Review 8.  Serotonin and beyond-a tribute to Manfred Göthert (1939-2019).

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Review 9.  Discriminating between 5-HT₃A and 5-HT₃AB receptors.

Authors:  A J Thompson; S C R Lummis
Journal:  Br J Pharmacol       Date:  2013-06       Impact factor: 8.739

Review 10.  5-HT(3) receptors.

Authors:  Sarah C R Lummis
Journal:  J Biol Chem       Date:  2012-10-04       Impact factor: 5.157
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