Target intelligence / Profile preview

Serotonin receptor (5-HTR) (5-HTR)

Target
5-HTR
Molecular classification
G protein-coupled receptor, Ligand-gated ion channel
01

Overview

Serotonin receptors, also known as 5-hydroxytryptamine (5-HT) receptors, are a diverse group of proteins that mediate the effects of the neurotransmitter serotonin across the central and peripheral nervous systems (StatPearls, 2023). This family consists of seven distinct classes (5-HT1 through 5-HT7), comprising 14 known subtypes; most are G protein-coupled receptors, with the exception of the 5-HT3 receptor, which is a ligand-gated ion channel (IUPHAR/BPS, 2024). These receptors play fundamental roles in regulating mood, cognition, perception, and various autonomic processes such as gastrointestinal motility and vascular tone (PubMed, 2022). While 5-HT1, 5-HT2, and 5-HT3 are the most common clinical targets, the other receptors like 5-HT4, 5-HT6, and 5-HT7 are increasingly targeted for cognitive enhancement and metabolic disorders (NIH, 2023). Therapeutic agents include agonists like triptans for migraines and antagonists like ondansetron for nausea, though careful selection is required to avoid off-target effects like serotonin syndrome or cardiovascular complications (PubChem, 2024).

Other names
5-hydroxytryptamine receptor5-HT receptorSerotonin receptor family
02

Mechanism of action

Agonism, antagonism, or partial agonism of specific 5-HT receptor subtypes to modulate intracellular signaling pathways (e.g., cAMP, IP3) or ion conductance (StatPearls, 2023).

03

Biological functions

Signal transductionNeurotransmissionRegulation of moodRegulation of sleepRegulation of appetiteGastrointestinal motility
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Disease associations

DepressionAnxiety disorderMigraineSchizophreniaIrritable bowel syndromeNausea and vomiting
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Safety considerations

Serotonin syndromeCardiac valvulopathyQT interval prolongationExtrapyramidal symptoms
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Interacting drugs

Sumatriptan

6 more in the full profile.

07

Biomarkers

5-Hydroxyindoleacetic acid (5-HIAA) levelsReceptor occupancy via Positron Emission Tomography (PET) imaging

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