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Encyclopedia of Signaling Molecules pp 5373–5377Cite as

The 5-HT3 Receptor

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Synonyms

5-HT; 5-Hydroxytryptamine; Serotonin

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), but it has become obvious over the years that 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 initiates its actions by binding to specific receptor proteins in the cell membrane. These 5-HT receptors were initially subdivided into D and M subtypes, based on their sensitivity to dibenyline or morphine (Gaddum and Picarelli 1957). This was an oversimplification, and currently 5-HT receptors are divided into seven major families (5-HT1–7) based on transduction and structural characteristics. All of these receptors exert their effects via G proteins, except for the 5-HT3receptor which is a ligand-gated ion channel (LGIC),...

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References

  • Barnes NM, Hales TG, Lummis SC, Peters JA. The 5-HT3 receptor--the relationship between structure and function. Neuropharmacology. 2009;56:273–84.

    Article  PubMed  CAS  Google Scholar 

  • Davies PA. Allosteric modulation of the 5-HT3 receptor. Curr Opin Pharmacol. 2011;11:75–80.

    Google Scholar 

  • 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.

    Article  PubMed  CAS  Google Scholar 

  • Gaddum JH, Picarelli ZP. Two kinds of tryptamine receptor. Br J Pharmacol Chemother. 1957;12:323–8.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Goyal R, Salahudeen AA, Jansen M. Engineering a prokaryotic Cys-loop receptor with a third functional domain. J Biol Chem. 2011;286:34635–42.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Hassaine G, Deluz C, Grasso L, Wyss R, Tol MB, Hovius R, Graff A, Stahlberg H, Tomizaki T, Desmyter A, Moreau C, Li XD, Poitevin F, Vogel H, Nury H. X-ray structure of the mouse serotonin 5-HT3 receptor. Nature. 2014;512:276–81.

    Article  PubMed  CAS  Google Scholar 

  • 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.

    Article  PubMed  CAS  Google Scholar 

  • Kelley SP, Dunlop JI, Kirkness EF, Lambert JJ, Peters JA. A cytoplasmic region determines single-channel conductance in 5-HT 3 receptors. Nature. 2003;424:321–4.

    Article  PubMed  CAS  Google Scholar 

  • Lummis SCR. 5-HT3 receptors. J. Biol. Chem. 2012;287:40239–45.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Machu TK. Therapeutics of 5-HT3 receptor antagonists: current uses and future directions. Pharmacol Ther. 2011;130:338–47.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Mawe GM, Hoffman JM. Serotonin signalling in the gut--functions, dysfunctions and therapeutic targets. Nat Rev Gastroenterol Hepatol. 2013;10:473–86.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Niesler B. 5-HT3 receptors: potential of individual isoforms for personalised therapy. Curr Opin Pharmacol. 2011;11:81–6.

    Article  PubMed  CAS  Google Scholar 

  • 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.

    Article  PubMed  CAS  Google Scholar 

  • Niesler B, Walstab J, Combrink S, Moller D, Kapeller J, Rietdorf J. Characterization of the novel human serotonin receptor subunits 5-HT3C,5-HT3D, and 5-HT3E. Mol Pharmacol. 2007;72:8–17.

    Article  PubMed  CAS  Google Scholar 

  • Nys M, Kesters D, Ulens C. Structural insights into Cys-loop receptor function and ligand recognition. Biochem Pharmacol. 2013;86:1042–53.

    Article  PubMed  CAS  Google Scholar 

  • Peters JA, Cooper MA, Carland JE, Livesey MR, Hales TG, Lambert JJ. Novel structural determinants of single channel conductance and ion selectivity in 5-hydroxytryptamine type 3 and nicotinic acetylcholine receptors. J Physiol. 2010;588:587–96.

    Article  PubMed  CAS  Google Scholar 

  • Rapport MM, Green A, Page IH. Purification of the substance which is responsible for the vasoconstrictor activity of serum. Fed Proc. 1947;6:184.

    PubMed  CAS  Google Scholar 

  • Thompson AJ, Lummis SCR. 5-HT3 receptors. Curr Pharm Des. 2006;12:3615–30.

    Google Scholar 

  • Thompson AJ, Lummis SCR. The 5-HT3 receptor as a therapeutic target. Expert Opin Ther Targets. 2007;11:527–40.

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Thompson AJ, Lester HA, Lummis SCR. The structural basis of function in Cys-loop receptors. Q Rev Biophys. 2010;43:449–99.

    Article  PubMed  CAS  Google Scholar 

  • Thompson AJ, Lummis SCR. Discriminating between 5-HT3A and 5-HT3AB receptors. Br J Pharmacol. 2013;169:736–747.

    Google Scholar 

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Author information

Authors and Affiliations

  1. Department of Biochemistry, University of Cambridge, Cambridge, CB2 1QW, UK

    Sarah C. R. Lummis

Authors
  1. Sarah C. R. Lummis
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Correspondence to Sarah C. R. Lummis .

Editor information

Editors and Affiliations

  1. Department of Molecular Science and Technology, Ajou University, Suwon, Korea

    Sangdun Choi

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Lummis, S.C.R. (2018). The 5-HT3 Receptor. In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, Cham. https://doi.org/10.1007/978-3-319-67199-4_647

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