Target intelligence / Profile preview

Serotonin 5-hydroxytryptamine receptor type 3 (5-HT3)

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

Overview

The 5-HT3 receptor is a ligand-gated ion channel that mediates fast excitatory neurotransmission in both the central and peripheral nervous systems. It is activated by serotonin and plays a role in various physiological processes including emesis, pain perception, anxiety, and gut motility. The receptor is a pentameric structure, primarily composed of 5-HT3A subunits, but can also form heteromers with 5-HT3B, 5-HT3C, 5-HT3D, and 5-HT3E subunits. Drugs targeting the 5-HT3 receptor, such as the "setrons", are commonly used as antiemetics.

Other names
5HT3 receptor5-HT3 receptorSerotonin receptor 3HTR3
02

Mechanism of action

Activation of the receptor by serotonin opens the cation-selective channel allowing Na+ and K+ influx, leading to neuronal depolarization and excitation.

03

Biological functions

Neuronal excitationNeurotransmitter releaseIon channel activityModulation of gut motilitySignal transduction
04

Disease associations

EmesisVomitingIrritable Bowel Syndrome (IBS)Anxiety disordersPain disordersDrug addiction
05

Safety considerations

QT prolongation (with some 5-HT3 antagonists)Potential for drug interactions
06

Interacting drugs

Serotonin

8 more in the full profile.

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