The C and E subunits of the serotonin 5-HT3 receptor subtly modulate electrical properties of the receptor.

  title={The C and E subunits of the serotonin 5-HT3 receptor subtly modulate electrical properties of the receptor.},
  author={Nor S Yaakob and D. Nguyen and Betty Exintaris and Helen R. Irving},
  journal={Biomedicine \& pharmacotherapy = Biomedecine \& pharmacotherapie},
  • N. Yaakob, D. Nguyen, +1 author H. Irving
  • Published 2018
  • Chemistry, Medicine
  • Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
Serotonin type 3 (5-hydroxytrptamine-3, 5-HT3) receptors are ligand-gated cation channels present in both central and peripheral nervous systems. In humans there are five different subunits (A, B, C, D and E) of 5-HT3 receptors which can form homomeric or heteromeric receptors that may account for discrepancies in patient responses to treatments. The present study commences characterisation of the profiles of human 5-HT3 receptors containing C and/or E subunits. Recombinant 5-HT3 receptors were… Expand
3 Citations
Visualising functional 5-HT3 receptors containing A and C subunits at or near the cell surface.
Examination of interactions of A and C subunits using 5-HT3 receptor subunits containing fluorescent protein inserts between the 3rd and 4th transmembrane spanning region shows that both A homomers and AC heteromers contribute to whole cell currents in response to 5- HT with minimal contribution from C homomers. Expand
Tapping into 5-HT3 Receptors to Modify Metabolic and Immune Responses
The potential for targeting 5-HT3 receptors in conditions involving metabolic or inflammatory disorders based on recent findings is assessed, underscoring the challenges and limitations of this approach. Expand
Invertebrate serotonin receptors: a molecular perspective on classification and pharmacology
  • A. Tierney
  • Biology, Medicine
  • Journal of Experimental Biology
  • 2018
An overview of heterologously expressed receptors is provided, which considers evolutionary relationships among them, classification based on these relationships and nomenclature that reflects classification, and transduction pathways and pharmacological profiles are compared. Expand


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5-HT3 receptors are membrane ion channels
The first recordings of currents through single ion channels activated by 5-HT3 receptors are reported, in excised membrane patches from neurons of the guinea pig submucous plexus, implying a role for 5- HT, and perhaps other amines, as a 'fast' synaptic transmitter. Expand
Co-expression of the 5-HT3B serotonin receptor subunit alters the biophysics of the 5-HT3 receptor.
Evidence is found in favor of a pivotal role of subunit composition of 5-HT(3) receptors in serotonergic transmission because receptor desensitization and resensitized massively affect amplitude, duration, and frequency of synaptic signaling. Expand
5-HT3 receptors.
The 5-HT(3) receptor is a member of the Cys-loop family of ligand-gated ion channels that is located in both the peripheral and central nervous systems and the pharmacophore is reasonably well understood. Expand
The 5-HT3B Subunit Confers Spontaneous Channel Opening and Altered Ligand Properties of the 5-HT3 Receptor*
It is shown that co-expression of the 5-HT3A and 5- HT3B receptor subunits in the human embryonic kidney (HEK) 293 cells results in a receptor that displays a low level of constitutive (or agonist-independent) activity and that the properties of ligands can be modified by receptor composition. Expand
The 5-HT3 receptor – the relationship between structure and function
The relationship between the structure and the function of the 5-HT3 receptor is reviewed, describing recent studies that have identified numerous HTR3A and H TR3B gene polymorphisms that impact upon 5- HT3 receptor function, or expression, and consider their relevance to (patho)physiology. Expand
Heterogeneity amongst 5-HT₃ receptor subunits: is this significant?
This review discusses the properties of the different subunits and their distribution to determine if they contribute to functional changes in the 5-HT₃ receptor and the implications of these findings with respect to drug design and tailored pharmacogenomic therapies. Expand
Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit.
A quantitative comparison of the pharmacological profiles of human and mouse recombinant 5-HT3R-AS receptor complexes revealed differences in the potencies of some antagonist or agonist compounds tested, the most dramatic example being (+)-tubocurarine, which demonstrated an approximately 1800-fold discrepancy in antagonist potency. Expand
Characterization of the Novel Human Serotonin Receptor Subunits 5-HT3C,5-HT3D, and 5-HT3E
Data show for the first time that the novel 5- HT3 subunits are able to form heteromeric 5-HT3 receptors, which exhibit quantitatively different functional properties compared with homomeric 4-HT2A and 3-HT1 receptors. Expand
The Pharmacological and Functional Characteristics of the Serotonin 5-HT3A Receptor Are Specifically Modified by a 5-HT3B Receptor Subunit*
The cloning of a subunit 5-HT3B with ∼44% amino acid identity to 5-ht3A that specifically modified 5- HT3Areceptor kinetics, voltage dependence, and pharmacology is reported, suggesting that 5-TT3B might contribute to tissue-specific functional changes in 5-Hat3-mediated signaling and/or modulation. Expand