Target intelligence / Profile preview

Serotonin Receptor 5-HT3 (5-HT3)

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

Overview

The serotonin 5-HT3 receptor is a ligand-gated ion channel that mediates fast excitatory neurotransmission in both the central and peripheral nervous systems. Upon binding serotonin, the channel opens, allowing the influx of cations like Na+, K+, and Ca2+, leading to neuronal depolarization. Antagonists of this receptor are clinically used as antiemetics and in the treatment of irritable bowel syndrome. The receptor is a pentamer composed of subunits including 5-HT3A, 5-HT3B, HTR3C, HTR3D, and HTR3E, which can form homo- or heteromeric channels. Genetic polymorphisms in the genes encoding these subunits can affect receptor expression and function.

Other names
5-hydroxytryptamine receptor 3HTR3
02

Mechanism of action

Antagonists bind to the receptor, blocking serotonin binding and preventing channel opening.

03

Biological functions

Fast excitatory neurotransmissionModulates neurotransmitter releaseSynaptic plasticityNeuronal excitation
04

Disease associations

Chemotherapy-induced nausea and vomitingIrritable Bowel SyndromeDepressionAnxiety
05

Interacting drugs

Ondansetron

2 more in the full profile.

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