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5-hydroxytryptamine receptors 3, 6, and 7 (5-HT3, 5-HT6, 5-HT7)

Target
5-HT3, 5-HT6, 5-HT7
Molecular classification
Ion channel, G protein-coupled receptor, Receptor
01

Overview

The 5-hydroxytryptamine (5-HT) receptors 3, 6, and 7 are a group of serotonin receptors that serve as significant therapeutic targets in neurology and psychiatry (NIH, 2023). The 5-HT3 receptor is a unique member of the family as it is a ligand-gated ion channel, whereas 5-HT6 and 5-HT7 are G protein-coupled receptors (Wikipedia, 2024). 5-HT3 receptors are primarily involved in rapid excitatory neurotransmission and the mediation of the emetic reflex, making their antagonists essential in treating chemotherapy-induced nausea (Drugs.com, 2024). 5-HT6 and 5-HT7 receptors are predominantly expressed in the central nervous system and play vital roles in regulating cognition, mood, and circadian rhythms (ACS, 2018; NIH, 2021). These receptors are collectively implicated in the pathophysiology of various neuropsychiatric conditions, including depression, schizophrenia, and Alzheimer's disease (ResearchGate, 2022). Drugs targeting these receptors, such as the multimodal antidepressant vortioxetine and various atypical antipsychotics, are used to manage complex conditions like major depressive disorder and cognitive deficits (NIH, 2021). Therapeutic modulation of these receptors aims to restore neurotransmitter balance and improve clinical outcomes in patients with mood and cognitive disorders (ACS, 2018). Overall, the 5-HT3, 6, and 7 receptors represent a diverse set of targets with broad clinical applications in both central and peripheral diseases (NIH, 2023).

Other names
Serotonin receptors 3, 6, and 75-HT3, 5-HT6, and 5-HT7 receptorsHTR3, HTR6, and HTR75-hydroxytryptamine receptor 35-hydroxytryptamine receptor 65-hydroxytryptamine receptor 7
02

Mechanism of action

Antagonism of 5-HT3, 5-HT6, and 5-HT7 receptors to modulate neurotransmitter release and signaling pathways (NIH, 2021; ACS, 2018).

03

Biological functions

Signal transductionNeurotransmissionCognitionCircadian rhythmEmesisGut motility
04

Disease associations

DepressionSchizophreniaAlzheimer's diseaseNauseaIrritable bowel syndromeCognitive impairment
05

Safety considerations

Serotonin syndromeConstipationQT prolongationSleep disturbancesCognitive side effects
06

Interacting drugs

Vortioxetine

8 more in the full profile.

07

Biomarkers

[11C]GSK215083 (PET ligand for 5-HT6)[11C]SB-269970 (PET ligand for 5-HT7)5-HT3 receptor expression levels

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