Target intelligence / Profile preview

5-hydroxytryptamine receptor 3 (5-HT3 receptor) (5-HT3R)

Target
5-HT3R
Molecular classification
Receptor, Ligand-gated ion channel, Ion channel
01

Overview

The 5-hydroxytryptamine receptor 3 (5-HT3 receptor) is a member of the serotonin receptor family and is unique among them as a ligand-gated ion channel (as opposed to the other G protein-coupled serotonin receptors). It is predominantly expressed in the central and peripheral nervous system, where it mediates fast excitatory neurotransmission in response to serotonin. The 5-HT3 receptor is involved in the regulation of nausea and vomiting, mood modulation, anxiety, and pain transmission. Antagonists of this receptor, such as mirtazapine and ondansetron, are used to treat conditions like major depressive disorder and chemotherapy-induced nausea and vomiting, respectively. Mirtazapine acts as a noncompetitive antagonist at this receptor, contributing to its antidepressant and anxiolytic effects by altering serotonergic neurotransmission.

Other names
5-HT3 receptorSerotonin receptor 3HTR35HT3R
02

Mechanism of action

Antagonists of the 5-HT3 receptor inhibit serotonin-mediated excitatory neurotransmission; mirtazapine is a noncompetitive antagonist. 5-HT3 antagonists block ion channel opening by serotonin (5-hydroxytryptamine), reducing neural transmission related to emesis and mood.

03

Biological functions

Signal transductionNeurotransmissionModulation of nausea and vomiting reflexes
04

Disease associations

Neuropsychiatric disorders (e.g., depression, anxiety)Nausea and vomiting (especially chemotherapy-induced)Irritable bowel syndromePain modulation (to a lesser extent)
05

Safety considerations

QT prolongation (notably with ondansetron and some other 5-HT3 antagonists)Constipation, headache, and dizziness with 5-HT3 antagonistsSedation, weight gain, and increased appetite with mirtazapine (mainly via H1 antagonism)Drug-drug interactions
06

Interacting drugs

Mirtazapine

6 more in the full profile.

07

Biomarkers

No established direct biomarkers specific for 5-HT3 receptor antagonist therapy in clinical practice (as of current knowledge).

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