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A triad of residues aligning to Thr-152, Glu-209, and Lys-211 in Htr3, appear to be involved in side-chain interactions near binding sites in Htr3a (subunit alpha) and muscle-type Chrna1. Data suggest that mutating Htr3a triad to that of Chrna1 increases binding affinity of nicotine to Htr3a. (Htr3 = 5-hydroxytryptamine/serotonin receptor; Chrna1 = cholinergic receptor nicotinic alpha polypeptide 1)
Results show that 5-HT3AR was expressed in GABAergic interneurons containing somatostatin or calretinin, and most strongly in the olfactory bulb, cerebral cortex, hippocampus, and amygdala. The pons, medulla, and spinal cord showed partial 5-HT3AR expression. Meanwhile, slight expression of 5-HT3AR was seen in the thalamus, hypothalamus, and midbrain; but no expression in the cerebellum.
Knock down serotonin receptors 5-HTR3 and 5-HTR4 in neonatal cardiomyocytes resulted in significant increase of cell damage in response to hypoxia, and also led to alternation in heart beating.
analysis of the structure from the full-length 5-HT3AR channel in the apo-state determined by single-particle cryo-electron microscopy
Transmission of sour taste information involves communication between taste cells and 5-HT3A-expressing afferent nerve fibers.
the recently available murine 5-HT3 receptor by identifying sites of strong interaction with particular functional groups at both the orthogonal (serotonin) site and a proposed allosteric binding site situated at the interface between the transmembrane region and the extracellular domain, was characterized.
We conclude that cholera toxin inhibits colonic migrating motor complexes via release of mucosal 5-HT, which activates an inhibitory pathway involving 5-HT3 receptors
It was concluded that epithelial 5-HT3 receptor may function as a mediator of gut microbiota-driven change in intestinal secretion.
5HT3A receptor deletion in neuroblasts impaired speed and directionality of migration and abolished calcium spikes.
The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors. Results demonstrate allosteric blockade by bupropion of the 5-HT3AR.
Studies with 16 arylguanidines found that their functional activity spanned a broad spectrum from superagonist to full agonist, partial agonist, and antagonist at 5-HT3 receptors; results confirm the utility of phenylguanidine as an extremely versatile scaffold in the design of 5-HT3 ligands with a "tunable" level of agonist or antagonist activity
5-HT3A-ICD is not only required but also sufficient for interaction with RIC-3
found the protein levels of AMPA receptor subunits (GluR1 and GluR2) are upregulated in the amygdala and the 5-HT3 receptor is downregulated in hypothalamic regions of Socially Isolated mice.
The data of this study demonstrated that the 5-HT3 receptor is the critical target of 5-HT action in exercise-induced hippocampal neurogenesis and antidepressant effects, but not in learning enhancement.
The deletion of Htr3a was related to fatal arrhythmias and sudden cardiac death during pregnancy, and its activation reversed the QT prolongation.
The results of this study suggested that 5-HT released from type III cells activates gustatory nerve fibers via 5-HT3 receptors, accounting for a significant proportion of the neural taste response.
Htr3a is required for controlling the migration and laminar positioning of reelin-expressing interneurons in the neocortex.
Deletion of the 5-HT3AR gene in transgenic mice abolished N-methyl-d-aspartate (NMDA) receptor (NMDAR)-dependent long-term depression (LTD) induced by low-frequency stimulation (LFS) in hippocampal CA1 synapses in slices.
5HT2AR and 5HT3AR were detected by RT-PCR techniques.
Results indicate that vestibular ganglion cells express functional 5-HT3 receptor channels (with 5-HT3a and 5-HT3b subunits) and might play a modulatory role in the peripheral vestibular nervous system
This study demonstrated that the C and E subunits when assembled as simple or complex heteromeric 5-HT3 receptors may alter efficacies of serotonin and clinically used antagonists.
Methylation status of the HTR3A gene in mothers is linked to maternal violence-related psychopathology, trauma-induced brain activation patterns, and child attachment disturbance during a sensitive period in the development of self-regulation.
This study did not found HTR3A play a major role in predicting Antipsychotic-Induced Weight Gain.
Methylation pattern changes in the 5-HTR3A gene were associated with suicidal behavior in borderline personality disorder, bipolar disorder, and attention deficit/hyperactivity disorder (ADHD).
findings suggest that HTR3A mRNA expression levels were positively correlated with craving in Han Chinese alcohol-dependent patients.
Study provides structural data showing the orientation of palonosetron in a 5-HT3 receptor binding site mimic, combined with functional data in the 5-HT3 receptor, provide an explanation for the high affinity and long-lived actions of this compound. These are likely due to specific interactions formed with binding site residues, and its location as a tight and effective wedge in the binding pocket.
Studies have demonstrated that 5-HT3 receptors modulate the activity of vascular and non-vascular smooth muscles.
The HTR3A rs1062613 polymorphisms do not seem to directly influence experimental muscle pain in healthy individuals. However, women reported higher pain intensity and larger pain area than men, which might partly be attributed to genotype.
Analysis of our small Chinese sample revealed a significant association of HTR3A with bipolar disorder, but yielded no evidence of an association between HTR3B and bipolar disorder. Furthermore, evidence for an association was found for a haplotype of HTR3A.
Alternative Viewpoint Against Breast Cancer Based on Selective Serotonin Receptors 5HTR3A and 5HTR2A Antagonists that can Mediate Apoptosis in MCF-7 Cell Line
Serotonin 3A receptor (5-HT3AR) is associated at the genetic and epigenetic levels with a variety of psychiatric disorders.
A gene-environment interaction is revealed between childhood trauma and 5-htr3a polymorphisms.
5-HT3A receptor distal targeting in axons and dendrites depends on P2X2R expression.
Agonist- and antagonist-induced up-regulation of surface 5-HT3 A receptors
Data indicate that no two n-alkanols act alike, their spectra of effects on serotonin receptor 3A (5-HT3A) receptors differ.
Our findings support the notion that different haplotypes of HTR3A have reciprocal effects in the etiology of Postoperative nausea.
HTR3A gene variants may contribute to variability in severity of and response to antiemetic therapy for nausea and vomiting of pregnancy.
These data support a role for intracellular salt bridges in maintaining the quaternary structure of the 5-HT3 receptor and suggest a role for the intracellular domain in allosteric modulation of cooperativity and agonist efficacy.
To conclude, considering 5-hydroxytryptamine 3A subtype receptor role in accomplishment of asthma symptoms, this increase in its expression may exacerbate the seriousness of asthma disease.
The product of this gene belongs to the ligand-gated ion channel receptor superfamily. This gene encodes subunit A of the type 3 receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor causes fast, depolarizing responses in neurons after activation. It appears that the heteromeric combination of A and B subunits is necessary to provide the full functional features of this receptor, since either subunit alone results in receptors with very low conductance and response amplitude. Alternatively spliced transcript variants encoding different isoforms have been identified.
5-hydroxytryptamine (serotonin) receptor 3A
, 5-hydroxytryptamine receptor 3A
, 5-HT3 receptor
, 5-hydroxytryptamine receptor 3A-like
, 5-hydroxytryptamine receptor 3
, 5HT3 serotonin receptor
, serotonin receptor 3A
, serotonin-gated ion channel receptor
, 5-HT3-Al receptor
, 5-hydroxytryptamine type 3A receptor