ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2007
Differential effects of serotonin and dopamine on human 5-HT3A receptor kinetics: interpretation within an allosteric kinetic model.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 48 citations in OpenAlex.
- HTR3A Receptor Signaling in Human Disease: From Bioelectrical Regulation to Therapeutic Targeting.Molecular neurobiology · 2026Review
- Role of 5-hydroxytryptamine type 3 receptors in the regulation of anxiety reactions.Journal of Zhejiang University. Science. B · 2024Article
- Efficiently Differentiating Agonists and Competitive Antagonists for Weak Allosteric Protein-Ligand Interactions with Linear Response Theory.ACS omega · 2023Article
- Fluorescent Nanozeolite Receptors for the Highly Selective and Sensitive Detection of Neurotransmitters in Water and Biofluids.Advanced materials (Deerfield Beach, Fla.) · 2021Article
- Structure, Function and Physiology of 5-Hydroxytryptamine Receptors Subtype 3.Sub-cellular biochemistry · 2021Review
- Orthosteric and Allosteric Activation of Human 5-HTBiophysical journal · 2020Article
- Evidence for an effect of receptor density on ligand occupancy and agonist ECScientific reports · 2019Article
- Novel mechanism of modulation at a ligand-gated ion channel; action of 5-Cl-indole at the 5-HTBritish journal of pharmacology · 2016Article
- Copper and protons directly activate the zinc-activated channel.Biochemical pharmacology · 2016Article
- Photoactivatable, biologically-relevant phenols with sensitivity toward 2-photon excitation.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2015Article
- αS-conotoxin GVIIIB potently and selectively blocks α9α10 nicotinic acetylcholine receptors.Biochemical pharmacology · 2015Article
- Unraveling mechanisms underlying partial agonism in 5-HT3A receptors.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- The structural mechanism of the Cys-loop receptor desensitization.Molecular neurobiology · 2013Review
- An outline of desensitization in pentameric ligand-gated ion channel receptors.Cellular and molecular life sciences : CMLS · 2013Review
- The pyrrole etomidate analog carboetomidate potently inhibits human 5-HT3A receptor function: comparisons with etomidate and potential implications for emetogenesis.Anesthesia and analgesia · 2013Article
- Macroscopic kinetics of pentameric ligand gated ion channels: comparisons between two prokaryotic channels and one eukaryotic channel.PloS one · 2013Article
- Comodulation of dopamine and serotonin on prefrontal cortical rhythms: a theoretical study.Frontiers in integrative neuroscience · 2013Article
- Article
- Allosteric modulation of the 5-HT(3) receptor.Current opinion in pharmacology · 2011Review
- A novel mechanism of modulation of 5-HT₃A receptors by hydrocortisone.Biophysical journal · 2011Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
Serotonin type 3 (5-HT3) receptors are members of the pentameric Cys-loop superfamily of receptors that modulate synaptic neurotransmission. In response to agonist binding and unbinding, members of this superfamily undergo a series of conformational transitions that define their functional properties. In this study, we report the results of electrophysiological studies using rapid solution exchange designed to characterize and compare the actions of the high-efficacy agonist serotonin and the low-efficacy agonist dopamine on human 5-HT3A receptors expressed in human embryonic kidney HEK293 cells. In the case of serotonin, receptor activation rates varied with agonist concentration, and deactivation occurred as a single-exponential process with a rate that was similar to the maximal rate of desensitization. Receptors recovered slowly from long desensitizing pulses of serotonin with a sigmoidal time course. In the case of dopamine, receptor activation rates were independent of agonist concentration, receptor deactivation occurred as a complex process that was significantly faster than the maximal rate of desensitization, and recovery from desensitization occurred more quickly than with 5-HT and its time course was not sigmoidal. We developed an allosteric kinetic model for 5-HT3A receptor activation, deactivation, desensitization, and resensitization. Interpretation of our results within the context of this model indicated that the distinct modulatory actions of serotonin versus dopamine are largely attributable to the vastly different rates with which these two agonists induce channel opening and dissociate from open and desensitized states.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.