Target intelligence / Profile preview

Serotonin 3 Receptor (5-HT3 receptor)

Target
5-HT3 receptor
Molecular classification
Ligand-gated ion channel, Cys-loop superfamily, Receptor
01

Overview

The 5-HT3 receptor is a ligand-gated ion channel that belongs to the Cys-loop superfamily. It's a cation-selective channel permeable to Na⁺ and K⁺, mediating fast excitatory neurotransmission. It is formed as a pentamer, either as a homopentamer of five identical 5-HT3A subunits or as heteropentamers combining the A subunit with one or more B, C, D, or E subunits. It is primarily known for its role in emesis and is targeted by "setron" antiemetics but is also implicated in pain, psychiatric, and gastrointestinal disorders.

Other names
5-hydroxytryptamine type-3 receptorHTR3AHTR3BHTR3CHTR3DHTR3E
02

Mechanism of action

Cation-selective channel permeable primarily to Na⁺ and K⁺ ions. Activation leads to rapid neuronal depolarization/excitation in both central and peripheral nervous systems by allowing cations to flow into neurons upon serotonin binding. Antagonists block this ion flow.

03

Biological functions

NeurotransmissionIon channel activityModulates neurotransmitter releaseFast excitatory synaptic transmissionNeuronal depolarization/excitation
04

Disease associations

Emesis/vomiting reflexesPain disordersPsychiatric disordersAnxietyDepressionSubstance abuseAddictionCognition-related diseasesGastrointestinal disordersIrritable bowel syndrome
05

Interacting drugs

Serotonin

12 more in the full profile.

06

Biomarkers

HTR3A polymorphismsHTR3B polymorphisms

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