Encyclopedia of Signaling Molecules

2012 Edition
| Editors: Sangdun Choi

The 5-HT3 Receptor

Reference work entry
DOI: https://doi.org/10.1007/978-1-4419-0461-4_647

Synonyms

Historical Background

5-Hydroxytryptamine (5-HT), also known as serotonin, was initially identified as a potent vasoconstrictor present in blood serum (Rapport et al. 1947). It is now clear 5-HT has a multitude of functions including activation or inhibition of muscle, exocrine and endocrine glands, central and peripheral neurons, and cells of the hematopoietic and immune systems. 5-HT receptors were initially subdivided into D and M subtypes, based on their sensitivity to dibenyline or morphine (Gaddum and Picarelli 1957). Currently, 5-HT receptors are divided into seven major families (5-HT1-7) based on transduction and structural characteristics. All are G-protein-coupled receptors, except for the 5-HT3 receptor which is a ligand-gated ion channel (LGIC), and indeed, it is this receptor which is the original M receptor.

Introduction

The 5-HT3receptor is a cation-selective member of the Cys-loop family of LGIC. The receptors are...

This is a preview of subscription content, log in to check access

References

  1. Bocquet N, Nury H, Baaden M, Le Poupon C, Changeux JP, Delarue M, Corringer PJ. X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation. Nature. 2009;457:111–14.PubMedGoogle Scholar
  2. Brejc K, van Dijk WJ, Klaassen RV, Schuurmans M, van Der Oost J, Smit AB, Sixma TK. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature. 2001;411:269–76.PubMedGoogle Scholar
  3. Davies PA, Pistis M, Hanna MC, Peters JA, Lambert JJ, Hales TG, Kirkness EF. The 5-HT3B subunit is a major determinant of serotonin-receptor function. Nature. 1999;397:359–63.PubMedGoogle Scholar
  4. Gaddum JH, Picarelli ZP. Two kinds of tryptamine receptor. Br J Pharmacol Chemother. 1957;12:323–8.PubMedGoogle Scholar
  5. Hibbs RE, Gouaux E. Principles of activation and permeation in an anion-selective Cys-loop receptor. Nature. 2011;474:54–60.PubMedGoogle Scholar
  6. Hilf RJ, Dutzler R. X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature. 2008;452:375–9.PubMedGoogle Scholar
  7. Hilf RJ, Dutzler R. Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel. Nature. 2009;457:115–18.PubMedGoogle Scholar
  8. Holbrook JD, Gill CH, Zebda N, et al. Characterisation of 5-HT3C, 5-HT3D and 5-HT3E receptor subunits: evolution, distribution and function. J Neurochem. 2009;108:384–96.PubMedGoogle Scholar
  9. Kelley SP, Dunlop JI, Kirkness EF, Lambert JJ, Peters JA. A cytoplasmic region determines single-channel conductance in 5-HT3 receptors. Nature. 2003;424:321–4.PubMedGoogle Scholar
  10. Niesler B, Frank B, Kapeller J, Rappold GA. Cloning, physical mapping and expression analysis of the human 5-HT3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E. Gene. 2003;310:101–11.PubMedGoogle Scholar
  11. Niesler B, Walstab J, Combrink S, et al. Characterization of the novel human serotonin receptor subunits 5-HT3C,5-HT3D, and 5-HT3E. Mol Pharmacol. 2007;72:8–17.PubMedGoogle Scholar
  12. Rapport MM, Green A, Page IH. Purification of the substance which is responsible for the vasoconstrictor activity of serum. Fed Proc. 1947;6:184.PubMedGoogle Scholar
  13. Reeves DC, Lummis SC. The molecular basis of the structure and function of the 5-HT3 receptor: a model ligand-gated ion channel (review). Mol Membr Biol. 2002;19:11–26.PubMedGoogle Scholar
  14. Thompson AJ, Lummis SC. 5-HT3 receptors. Curr Pharm Des. 2006;12:3615–30.PubMedGoogle Scholar
  15. Thompson AJ, Lummis SC. The 5-HT3 receptor as a therapeutic target. Expert Opin Ther Targets. 2007;11:527–40.PubMedGoogle Scholar
  16. Thompson AJ, Lester HA, Lummis SC. The structural basis of function in Cys-loop receptors. Q Rev Biophys. 2010;43:449–99.PubMedGoogle Scholar

Copyright information

© Springer Science+Business Media, LLC 2012

Authors and Affiliations

  1. 1.Department of BiochemistryUniversity of CambridgeCambridgeUK