The 5-HT3 receptor – the relationship between structure and function

Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors

2001 • 1,736 citations

Refined Structure of the Nicotinic Acetylcholine Receptor at 4Å Resolution

2004 • 1,626 citations

Structure and gating mechanism of the acetylcholine receptor pore

2003 • 1,261 citations

Primary Structure And Functional Expression of the 5HT ₃ Receptor, A Serotonin-gated Ion Channel

1991 • 976 citations

Emerging structure of the Nicotinic Acetylcholine receptors

2002 • 896 citations

Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance

1988 • 798 citations

Nicotine and Carbamylcholine Binding to Nicotinic Acetylcholine Receptors as Studied in AChBP Crystal Structures

2004 • 778 citations

X-ray structure of a prokaryotic pentameric ligand-gated ion channel

2008 • 657 citations

5-HT3 receptors are membrane ion channels

1989 • 630 citations

A nomenclature for ligand-gated ion channels

2008 • 577 citations

The 5-HT3B subunit is a major determinant of serotonin-receptor function

1999 • 555 citations

From ab initio quantum mechanics to molecular neurobiology: A cation–π binding site in the nicotinic receptor

1998 • 544 citations

Amphipathic analysis and possible formation of the ion channel in an acetylcholine receptor.

1984 • 513 citations

Recent advances in Cys-loop receptor structure and function

2006 • 505 citations

Nicotinic acetylcholine receptor at 4.6 Å resolution: transverse tunnels in the channel 1 1Edited by J. Karn

1999 • 487 citations

Cys-loop receptors: new twists and turns

2004 • 426 citations

Chimaeric nicotinic–serotonergic receptor combines distinct ligand binding and channel specificities

1993 • 401 citations

Crystal structure of the extracellular domain of nAChR α1 bound to α-bungarotoxin at 1.94 Å resolution

2007 • 395 citations

Mutations at two distinct sites within the channel domain M2 alter calcium permeability of neuronal alpha 7 nicotinic receptor.

1993 • 389 citations

Nervous system distribution of the serotonin 5-HT3 receptor mRNA.

1993 • 369 citations

The 5-HT₃Receptor Is Present in Different Subpopulations of GABAergic Neurons in the Rat Telencephalon

1997 • 363 citations

A prokaryotic proton-gated ion channel from the nicotinic acetylcholine receptor family

2006 • 302 citations

Cation−π Interactions in Ligand Recognition by Serotonergic (5-HT_3A) and Nicotinic Acetylcholine Receptors: The Anomalous Binding Properties of Nicotine

2002 • 297 citations

The Pharmacological and Functional Characteristics of the Serotonin 5-HT3A Receptor Are Specifically Modified by a 5-HT3B Receptor Subunit

1999 • 278 citations

A cytoplasmic region determines single-channel conductance in 5-HT3 receptors

2003 • 273 citations

Cloning, physical mapping and expression analysis of the human 5-HT3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E

2003 • 245 citations

Activation of Serotonin Receptors Modulates Synaptic Transmission in Rat Cerebral Cortex

1999 • 241 citations

Serotonin facilitates GABAergic transmission in the CA1 region of rat hippocampus in vitro.

1991 • 231 citations

The 5-HT₃receptor as a therapeutic target

2007 • 228 citations

Genetic manipulation of ion channels: A new approach to structure and mechanism

1989 • 223 citations

5-HT₃Receptors Mediate Serotonergic Fast Synaptic Excitation of Neocortical Vasoactive Intestinal Peptide/Cholecystokinin Interneurons

2002 • 211 citations

5-HT3 Receptors

2006 • 206 citations

Ligand-gated ion channels: mechanisms underlying ion selectivity

2003 • 196 citations

Fast Synaptic Signaling by Nicotinic Acetylcholine and Serotonin 5-HT₃Receptors in Developing Visual Cortex

1997 • 194 citations

Ca²⁺Permeability of the (α4)₃(β2)₂Stoichiometry Greatly Exceeds That of (α4)₂(β2)₃Human Acetylcholine Receptors

2006 • 193 citations

5-hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala

1992 • 192 citations

The molecular basis of the structure and function of the 5-HT 3 receptor: a model ligand-gated ion channel (Review)

2002 • 188 citations

Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.

1995 • 179 citations

Differential Composition of 5-Hydroxytryptamine₃Receptors Synthesized in the Rat CNS and Peripheral Nervous System

2002 • 177 citations

The selective vulnerability of nerve cells in Huntington's disease

2001 • 176 citations

Quantitative autoradiographic mapping of 5‐HT₃ receptors in the rat CNS using [¹²⁵I]iodo‐zacopride and [³H]zacopride as radioligands

1992 • 165 citations

5-Hydroxytryptamine3 receptors in the human brain: Autoradiographic visualization using [3H]ICS 205-930

1989 • 158 citations

Variations in the 5-Hydroxytryptamine Type 3B Receptor Gene as Predictors of the Efficacy of Antiemetic Treatment in Cancer Patients

2003 • 157 citations

The 5-HT3 receptor ligand, [3H]BRL 43694, binds to presynaptic sites in the nucleus tractus solitarius of the rat

1989 • 150 citations

A Novel Class of Ligand-gated Ion Channel Is Activated by Zn2+

2003 • 149 citations

Location of a threonine residue in the α -subunit M2 transmembrane segment that determines the ion flow through the acetylcholine receptor channel

1991 • 148 citations

Cloning and fnctional expression of an apparent splice variant of the murine 5-HT3 receptor A subunit

1993 • 147 citations

Characterization of the Novel Human Serotonin Receptor Subunits 5-HT_3C,5-HT_3D, and 5-HT_3E

2007 • 145 citations

Hippocampal Interneurons Are Excited Via Serotonin-Gated Ion Channels

1997 • 141 citations

Acetylcholine receptor channel structure in the resting, open, and desensitized states probed with the substituted-cysteine-accessibility method

2001 • 137 citations

Central and peripheral 5-HT3 receptors

1992 • 137 citations

Ultrastructure of the 5‐Hydroxytryptamine₃ Receptor

1995 • 132 citations

Single amino acid substitution affects desensitization of the 5-hydroxytryptamine type 3 receptor expressed in Xenopus oocytes.

1993 • 130 citations

Association between the 5′ UTR variant C178T of the serotonin receptor gene HTR3A and bipolar affective disorder

2001 • 129 citations

Expression of Recombinant Homo-oligomeric 5-Hydroxytryptamine3 Receptors Provides New Insights into Their Maturation and Structure

1995 • 129 citations

Characterisation and autoradiographic localisation of 5-HT3 receptor recognition sites identified with [3H]-(S)-zacopride in the forebrain of the rat

1990 • 128 citations

Conversion of the Ion Selectivity of the 5-HT3AReceptor from Cationic to Anionic Reveals a Conserved Feature of the Ligand-gated Ion Channel Superfamily

2001 • 127 citations

A ring of uncharged polar amino acids as a component of channel constriction in the nicotinic acetylcholine receptor

1991 • 127 citations

Rings of anionic amino acids as structural determinants of ion selectivity in the acetylcholine receptor channel

1991 • 127 citations

Consensus meeting agrees distribution of 5-HT3 receptors in mammalian hindbrain

1990 • 124 citations

Differential subcellular localization of the 5‐HT₃‐A_s receptor subunit in the rat central nervous system

2002 • 123 citations

Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit.

1995 • 117 citations

Structural model of nicotinic acetylcholine receptor isotypes bound to acetylcholine and nicotine.

2002 • 116 citations

Modular Design of Cys-loop Ligand-gated Ion Channels: Functional 5-HT3 and GABA ρ1 Receptors Lacking the Large Cytoplasmic M3M4 Loop

2008 • 113 citations

Ion permeation and conduction in a human recombinant 5‐HT₃ receptor subunit (h5‐HT_3A)

1998 • 109 citations

Prolyl isomerase requirement for the expression of functional homo-oligomeric ligand-gated ion channels

1994 • 108 citations

Atomic force microscopy reveals the stoichiometry and subunit arrangement of 5-HT₃receptors

2005 • 107 citations

Dual Role of the RIC-3 Protein in Trafficking of Serotonin and Nicotinic Acetylcholine Receptors

2005 • 106 citations

Distribution and functional properties of 5-HT3 receptors in the rat hippocampal dentate gyrus: a patch-clamp study

1994 • 100 citations

Prediction of 5-HT3 Receptor Agonist-Binding Residues Using Homology Modeling

2003 • 99 citations

High Calcium Permeability of Serotonin 5‐HT₃ Receptors on Presynaptic Nerve Terminals from Rat Striatum

1998 • 96 citations

Evidence for Expression of Heteromeric Serotonin 5-HT3 Receptors in Rodents

2000 • 95 citations

Common Determinants of Single Channel Conductance within the Large Cytoplasmic Loop of 5-Hydroxytryptamine Type 3 and α4β2 Nicotinic Acetylcholine Receptors

2006 • 95 citations

Tyrosine Residues That Control Binding and Gating in the 5-Hydroxytryptamine₃Receptor Revealed by Unnatural Amino Acid Mutagenesis

2004 • 95 citations

Serotonin 5-HT3 receptors in the central nervous system

2006 • 95 citations

Presynaptic 5‐HT₃ receptor‐mediated modulation of synaptic GABA release in the mechanically dissociated rat amygdala neurons

2000 • 92 citations

Identification and Characterisation of 5‐Hydroxytryptamine₃ Recognition Sites in Human Brain Tissue

1989 • 92 citations

5-HT3 receptor channels in dissociated rat superior cervical ganglion neurons.

1992 • 91 citations

The Role of Tryptophan Residues in the 5-Hydroxytryptamine3 Receptor Ligand Binding Domain

2000 • 91 citations

Molecular Cloning, Functional Expression, and Pharmacological Characterization of 5-Hydroxytryptamine₃ Receptor cDNA and Its Splice Variants from Guinea Pig

1998 • 90 citations

Electrophysiology of 5-HT3 receptors in neuronal cell lines

1989 • 88 citations

Serotonin Excites Neurons in the Human Submucous Plexus via 5-HT3 Receptors

2005 • 87 citations

A cluster of novel serotonin receptor 3-like genes on human chromosome 3

2003 • 86 citations

Structural Features of the Ligand-binding Domain of the Serotonin 5HT3 Receptor

1999 • 85 citations

Calcium influx through presynaptic 5-HT3 receptors facilitates GABA release in the hippocampus: in vitro slice and synaptosome studies

2004 • 84 citations

Assembly and Cell Surface Expression of Homomeric and Heteromeric 5-HT3 Receptors: The Role of Oligomerization and Chaperone Proteins

2002 • 84 citations

Structural and Electrostatic Properties of the 5-HT3Receptor Pore Revealed by Substituted Cysteine Accessibility Mutagenesis

2001 • 83 citations

Autoradiographic distribution of [ 3 H]-(S)-zacopride-labelled 5-HT 3 receptors in human brain

1996 • 82 citations

Expression and function of 5-HT₃receptors in the enteric neurons of mice lacking the serotonin transporter

2002 • 82 citations

Synaptic activation and properties of 5-hydroxytryptamine(3) receptors in myenteric neurons of guinea pig intestine.

1999 • 79 citations

A Variant C178T in the Regulatory Region of the Serotonin Receptor GeneHTR3AModulates Neural Activation in the Human Amygdala

2005 • 77 citations

Evidence for a Centrally Located Gate in the Pore of a Serotonin-Gated Ion Channel

2002 • 77 citations

Analysis of the Ligand Binding Site of the 5-HT 3 Receptor Using Site Directed Mutagenesis: Importance of Glutamate 106

1997 • 77 citations

Locating an Antagonist in the 5-HT3 Receptor Binding Site Using Modeling and Radioligand Binding

2005 • 74 citations

Molecular determinants of single-channel conductance and ion selectivity in the Cys-loop family: insights from the 5-HT3 receptor

2005 • 74 citations

Organization of the mouse 5-HT3 receptor gene and functional expression of two splice variants

1994 • 73 citations

A distinct distribution of functional presynaptic 5-HT receptor subtypes on GABAergic nerve terminals projecting to single hippocampal CA1 pyramidal neurons

2003 • 72 citations

Serotonin type 3 receptor genes: HTR3A, B, C, D, E

2008 • 72 citations

High-frequency HTR3B variant associated with major depression dramatically augments the signaling of the human 5-HT _3AB receptor

2008 • 72 citations

The effect of 5-hydroxytryptamine 3A and 3B receptor genes on nausea induced by paroxetine

2006 • 71 citations

Cell Surface Expression of 5-Hydroxytryptamine Type 3 Receptors Is Promoted by RIC-3

2005 • 70 citations

Direct Observation of Serotonin 5‐HT₃ Receptor‐Induced Increases in Calcium Levels in Individual Brain Nerve Terminals

1996 • 69 citations

Different Residues in the GABAA Receptor α1T60-α1K70 Region Mediate GABA and SR-95531 Actions

2002 • 67 citations

Distribution and characterization of the [3H]granisetron-labelled 5-HT3 receptor in the human forebrain

1993 • 66 citations

3B but which 3B? And that's just one of the questions: the heterogeneity of human 5-HT3 receptors

2008 • 66 citations

Desperately seeking subunits: are native 5-HT3 receptors really homomeric complexes?

1998 • 65 citations

Activation and desensitization of the 5‐HT3 receptor in a rat glioma x mouse neuroblastoma hybrid cell.

1991 • 65 citations

Peptidyl prolyl cis-trans isomerase activity of cyclophilin A in functional homo-oligomeric receptor expression

1997 • 62 citations

5‐HT₃‐receptor subunits A and B are co‐expressed in neurons of the dorsal root ganglion

2001 • 61 citations

Partial cDNA cloning and NGF regulation of a rat 5-HT3 receptor subunit

1993 • 61 citations

Serotonin receptor gene HTR3A variants in schizophrenic and bipolar affective patients.

2001 • 61 citations

Modified 5-HT3A receptor function by co-expression of alternatively spliced human 5-HT3A receptor isoforms

2000 • 60 citations

The role of central 5‐HT₃ receptors in vagal reflex inputs to neurones in the nucleus tractus solitarius of anaesthetized rats

2005 • 59 citations

Tissue-specific alternative promoters of the serotonin receptor gene HTR3B in human brain and intestine

2006 • 59 citations

Genetic polymorphisms in the 5-hydroxytryptamine type 3B receptor gene and paroxetine-induced nausea

2007 • 59 citations

A single ring of charged amino acids at one end of the pore can control ion selectivity in the 5‐HT₃ receptor

2003 • 57 citations

Probing the role of a conserved M1 proline residue in 5-hydroxytryptamine(3) receptor gating.

2000 • 57 citations

Polymorphisms in the novel serotonin receptor subunit gene HTR3C show different risks for acute chemotherapy-induced vomiting after anthracycline chemotherapy

2008 • 57 citations

Antibodies against the extracellular domain of the 5-HT3 receptor label both native and recombinant receptors

1999 • 56 citations

Pharmacological and Regional Characterization of [³H]LY278584 Binding Sites in Human Brain

1993 • 56 citations

Noninvasive Imaging of 5-HT3 Receptor Trafficking in Live Cells

2004 • 56 citations

Activation of presynaptic 5-HT3 receptors facilitates glutamatergic synaptic inputs to area postrema neurons in rat brain slices

2004 • 54 citations

Investigation of the human serotonin receptor gene HTR3B in bipolar affective and schizophrenic patients

2004 • 53 citations

Mutagenesis and Molecular Modeling Reveal the Importance of the 5-HT3 Receptor F-loop

2006 • 53 citations

5-Hydroxytryptamine-3 receptors modulate synaptic activity in the rat nucleus tractus solitarius in vitro

1992 • 53 citations

Immunolabeling of the rat central nervous system with antibodies partially selective of the short form of the 5-HT3 receptor

1999 • 52 citations

Structural Determinants of Ca2+ Permeability and Conduction in the Human 5-Hydroxytryptamine Type 3A Receptor

2008 • 52 citations

Cell Surface Expression of 5-Hydroxytryptamine Type 3 Receptors Is Controlled by an Endoplasmic Reticulum Retention Signal

2003 • 51 citations

Open probability of homomeric murine 5‐HT_3A serotonin receptors depends on subunit occupancy

2001 • 51 citations

[3H]ICS 205-930 labels 5-HT3 recognition sites in membranes of cat and rabbit vagus nerve and superior cervical ganglion

1989 • 50 citations

Pharmacological characterization of the apparent splice variants of the murine 5-HT3 R-A subunit expressed in Xenopus laevis oocytes

1994 • 49 citations

5-HT3 receptors in the CNS: 3B or not 3B?

2003 • 49 citations

Binding Interactions of Antagonists with 5‐Hydroxytryptamine_3AReceptor Models

2003 • 49 citations

A Hydrogen Bond in Loop A Is Critical for the Binding and Function of the 5-HT₃ Receptor

2008 • 49 citations

The Role of Tyrosine Residues in the Extracellular Domain of the 5-Hydroxytryptamine3 Receptor

2004 • 49 citations

An electrophysiological investigation of the properties of 5‐HT₃ receptors of rabbit nodose ganglion neurones in culture

1993 • 48 citations

Differential Effects of Serotonin and Dopamine on Human 5-HT_3AReceptor Kinetics: Interpretation within an Allosteric Kinetic Model

2007 • 47 citations

Molecular Determinants of Picrotoxin Inhibition of 5-Hydroxytryptamine Type 3 Receptors

2005 • 47 citations

Properties of 5‐hydroxytryptamine₃ receptor‐gated currents in adult rat dorsal root ganglion neurones

1991 • 47 citations

Labelling of 5-HT3 receptor recognition sites in the rat brain using the agonist radioligand [3H]meta-chlorophenylbiguanide

1993 • 45 citations

Differential Subcellular Localization of RIC-3 Isoforms and Their Role in Determining 5-HT3 Receptor Composition

2007 • 45 citations

Contributions of Torpedo Nicotinic Acetylcholine Receptor γTrp-55 and δTrp-57 to Agonist and Competitive Antagonist Function

2001 • 44 citations

Spatial Orientation of the Antagonist Granisetron in the Ligand-Binding Site of the 5-HT₃ Receptor

2005 • 44 citations

Naturally occurring variations in the human 5-HT3A gene profoundly impact 5-HT3 receptor function and expression

2007 • 44 citations

Contributions of the non‐α subunit residues (loop D) to agonist binding and channel gating in the muscle nicotinic acetylcholine receptor

2002 • 42 citations

Modulation of 5-HT3 Receptor-mediated Response and Trafficking by Activation of Protein Kinase C

2003 • 42 citations

Reduced levels of 5-HT3 receptor recognition sites in the putamen of patients with Huntington's disease

1993 • 41 citations

Molecular Determinants of (+)-Tubocurarine Binding at Recombinant 5-Hydroxytryptamine_3AReceptor Subunits

1999 • 41 citations

Presynaptic 5‐HT₃ receptors evoke an excitatory response in dorsal vagal preganglionic neurones in anaesthetized rats

1998 • 39 citations

Cloning and expression of ligand-gated ion-channel receptor L2 in central nervous system

2005 • 38 citations

The Role and Predicted Propensity of Conserved Proline Residues in the 5-HT3 Receptor

2001 • 38 citations

Characterization of the Ligand-binding Site of the Serotonin 5-HT3 Receptor

2003 • 38 citations

An Interaction Involving an Arginine Residue in the Cytoplasmic Domain of the 5-HT3A Receptor Contributes to Receptor Desensitization Mechanism

2006 • 35 citations

Potentiation of 5-HT3 receptor-mediated responses by protein kinase C activation

1995 • 35 citations

Identification of critical residues in loop E in the 5-HT3ASR binding site.

2002 • 34 citations

Identification of 5-HT3A and 5-HT3B receptor subunits in human hippocampus

2007 • 34 citations

Ligand-Induced 5-HT3 Receptor Internalization in Enteric Neurons in Rat Ileum

2006 • 34 citations

Defining the roles of Asn-128, Glu-129 and Phe-130 in loop A of the 5-HT₃receptor

2006 • 33 citations

Generation of a selective 5-HT3B subunit-recognising polyclonal antibody; identification of immunoreactive cells in rat hippocampus

2001 • 33 citations

Identification and importance of N-glycosylation of the human 5-hydroxytryptamine3A receptor subunit

2004 • 33 citations

The 4′lysine in the putative channel lining domain affects desensitization but not the single‐channel conductance of recombinant homomeric 5‐HT_3A receptors

2000 • 31 citations

Interactions of Granisetron with an Agonist-Free 5-HT_3A Receptor Model

2006 • 30 citations

Detection of human and rodent 5-HT3Breceptor subunits by anti-peptide polyclonal antibodies

2006 • 30 citations

Uropathic Observations in Mice Expressing a Constitutively Active Point Mutation in the 5-HT_3AReceptor Subunit

2004 • 28 citations

Dynamic Modification of a Mutant Cytoplasmic Cysteine Residue Modulates the Conductance of the Human 5-HT3A Receptor

2007 • 28 citations

Three putative N‐glycosylation sites within the murine 5‐HT3_A receptor sequence affect plasma membrane targeting, ligand binding, and calcium influx in heterologous mammalian cells

2004 • 28 citations

Cloning, expression, and characterization of ferret 5-HT3 receptor subunit

2000 • 26 citations

Immunolabelling of the 5‐HT_3B receptor subunit in the central and peripheral nervous systems in rodents

2007 • 26 citations

Single channel properties of the 5-HT3 subtype of serotonin receptor in primary cultures of rodent hippocampus

1994 • 25 citations

The distribution of 5-HT3 recognition sites in the marmoset brain

1992 • 25 citations

Identification of a domain affecting agonist potency of meta-chlorophenylbiguanide in 5-HT3 receptors

1999 • 25 citations

Native and Cloned 5-HT3A(S) Receptors Are Anchored to F-Actin in Clonal Cells and Neurons

2002 • 25 citations

A Mutation in Transmembrane Domain II of the 5-Hydroxytryptamine_3A Receptor Stabilizes Channel Opening and Alters Alcohol Modulatory Actions

2003 • 25 citations

Distinct subcellular targeting of fluorescent nicotinic α3β4 and serotoninergic 5‐HT_3A receptors in hippocampal neurons

2004 • 24 citations

Characterization of 5-HT<sub>3</sub> Receptor Mutations Identified in Schizophrenic Patients

2006 • 24 citations

Minimal Structural Rearrangement of the Cytoplasmic Pore during Activation of the 5-HT3A Receptor

2004 • 24 citations

Different efficacy of specific agonists at 5‐HT₃ receptor splice variants: the role of the extra six amino acid segment

1998 • 23 citations

Role of aspartate 298 in mouse 5‐HT_3A receptor gating and modulation by extracellular Ca²⁺

2005 • 23 citations

Functional characterization of a -100_-102delAAG deletion-insertion polymorphism in the promoter region of the HTR3B gene

2008 • 23 citations

Amino acids in transmembrane domain two influence anesthetic enhancement of serotonin-3A receptor function

2003 • 23 citations

Assignment of a Human Homolog of the Mouse Htr3 Receptor Gene to Chromosome 11q23.1-q23.2

1995 • 22 citations

Functional differences between splice variants of the murine 5-HT3A receptor: possible role for phosphorylation

2000 • 20 citations

Molecular cloning and pharmacological characterization of serotonin 5-HT3A receptor subtype in dog

2006 • 19 citations

Native Serotonin 5‐HT₃ Receptors Expressed in Xenopus Oocytes Differ from Homopentameric 5‐HT₃ Receptors

1997 • 18 citations

Functional group interactions of a 5-HT3R antagonist.

2002 • 17 citations

Casein kinase ii (protein kinase ck2) regulates serotonin 5-ht3 receptor channel function in ng108-15 cells

2003 • 16 citations

Pharmacological and electrophysiological properties of the naturally occurring Pro391Arg variant of the human 5-HT3A receptor

2004 • 16 citations

Comparison of [3H]YM060 binding to native and cloned rat 5-HT3 receptors

1996 • 13 citations

Do polymorphisms in the human 5-HT3 genes contribute to pathological phenotypes?

2006 • 12 citations

Phosphorylation of the 5-hydroxytryptamine3 (5-HT3) receptor expressed in HEK293 cells.

2000 • 12 citations