Target intelligence / Profile preview

Serotonin 5-hydroxytryptamine receptor 3A (5-HT3A)

Target
5-HT3A
Molecular classification
Receptor, Ligand-gated ion channel, Cys-loop family of ligand-gated ion channels
01

Overview

The serotonin 5-hydroxytryptamine receptor 3A (5-HT3A) is a subunit of the type 3 serotonin receptor, which is a ligand-gated ion channel. This receptor plays key roles in neurotransmission and is involved in various physiological and pathophysiological processes, including emesis control, cognition modulation, and anxiety regulation. The functional receptor can be formed as a homopentamer of five identical 5-HT3A subunits or as a heteropentamer with other related subunits. Upon binding serotonin, the channel opens to allow cations to flow into neurons, leading to depolarization. Selective antagonists, known as "setrons," are used clinically to prevent chemotherapy-induced nausea/vomiting by blocking this receptor's activity.

02

Mechanism of action

Antagonism; stabilization of non-conductive conformational states of the channel that block activation by endogenous ligands like serotonin.

03

Biological functions

Fast excitatory neurotransmissionModulates release of multiple transmittersNeurotransmission
04

Disease associations

EmesisAnxietyCognitive disorders
05

Interacting drugs

Ondansetron

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