Target intelligence / Profile preview

Serotonin Receptor-Ion Channel Complex (5-HT3 Receptor)

Target
5-HT3 Receptor
Molecular classification
Ligand-gated ion channel, Receptor
01

Overview

The serotonin receptor-ion channel complex, primarily referring to the 5-HT3 receptor, is a unique ligand-gated ion channel that mediates rapid excitatory neurotransmission. Upon serotonin binding, it opens a cation-selective pore, leading to neuronal depolarization. It plays a role in nausea/vomiting reflexes, gut motility, and modulation of pain pathways, with antagonists used as antiemetics.

Other names
5-Hydroxytryptamine Receptor 35-HT3Serotonin-gated ion channel
02

Mechanism of action

Ligand binding opens a cation-selective pore, leading to neuronal depolarization and excitation.

03

Biological functions

NeurotransmissionSynaptic transmissionIon channel activityRegulation of gut motilityModulation of pain pathways
04

Disease associations

NauseaVomitingIrritable Bowel Syndrome (IBS)AnxietyDepression
05

Safety considerations

QT prolongation (with some antagonists)Constipation (with some antagonists, particularly alosetron)Serotonin syndrome (rare, with concomitant serotonergic drugs)
06

Interacting drugs

Ondansetron

4 more in the full profile.

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