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

Target: 5-HT3
Molecular classification: Ligand-gated ion channel, Cation-selective channel, Cys-loop receptor superfamily

Overview

The 5-HT3 receptor is a ligand-gated ion channel mediating fast excitatory neurotransmission in both the central and peripheral nervous systems. It is activated by serotonin, leading to neuronal depolarization via cation influx. Unlike other serotonin receptors, it is not a G-protein-coupled receptor. It plays a role in various physiological processes including emesis, pain processing, reward, cognition, anxiety, and gastrointestinal motility, making it a target for antiemetic drugs and other therapeutic interventions. Genetic variability can impact drug response.

Other names: 5-HT3 receptor5-hydroxytryptamine type 3 receptor

Mechanism of action

Antagonism of 5-HT3 receptor-mediated ion flux

Biological functions

Fast excitatory neurotransmissionNeuronal depolarizationModulation of neurotransmitter releaseSynaptic plasticity

Disease associations

EmesisPainAnxietyGastrointestinal motility disordersReward system dysfunctionCognitive impairment

Safety considerations

Potential for drug interactions due to diverse pharmacologyVariability in drug response due to genetic polymorphisms

Interacting drugs

Serotonin

8 more in the full profile.

Biomarkers

Polymorphisms in HTR3A/B/C/D/E genes affecting function/expression/pharmacological response

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