Target intelligence / Profile preview

Serotonin 5-HT6 Receptor (5-HT6)

Target: 5-HT6
Molecular classification: G protein-coupled receptor, GPCR, Class A GPCR, Receptor

Overview

The serotonin 5HT6 receptor (5-HT6R) is a G protein-coupled receptor that binds serotonin and is primarily expressed in the central nervous system. It is coupled to Gs proteins, stimulating adenylate cyclase and increasing cAMP levels. It plays a role in cognition, memory, motor control, and emotional regulation. Antagonists have shown pro-cognitive effects by modulating cholinergic and glutamatergic neurotransmission. Polymorphisms in the HTR6 gene are associated with neuropsychiatric disorders.

Other names: 5HT6 receptorHTR65-hydroxytryptamine receptor 6ST-B17

Mechanism of action

Gs protein activation, Adenylyl cyclase activation, Increased cAMP levels, Modulation of acetylcholine and glutamate release

Biological functions

Signal transductionNeurotransmissionCognitionMemoryMotor controlEmotional regulationModulation of neurotransmitter release (acetylcholine, glutamate)

Disease associations

Cognitive disordersAlzheimer's diseaseParkinson's diseaseNeuropsychiatric disorders

Safety considerations

Potential for off-target effects due to GPCR promiscuityLimited understanding of long-term effects of chronic modulationPossible contribution to neuropsychiatric disease mechanisms

Interacting drugs

Atypical antipsychotics

3 more in the full profile.

Biomarkers

HTR6 gene polymorphisms (e.g., C267T (rs1805054)) as susceptibility markers

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