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Target intelligence / Profile preview
Serotonin 5-hydroxytryptamine Receptor Subtype Six (None)
- Target
- None
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The serotonin 5-HT6 receptor is a subtype of serotonin (5-hydroxytryptamine, 5-HT) receptor. It is a G protein-coupled receptor (GPCR), encoded by the HTR6 gene in humans. The 5-HT6 receptor binds the endogenous neurotransmitter serotonin and mediates excitatory neurotransmission via coupling to Gs proteins, which stimulate adenylate cyclase and increase intracellular cAMP levels. Its expression is almost exclusive to the central nervous system (CNS), particularly in regions associated with motor control, emotionality, cognition, learning, and memory. It is considered an attractive therapeutic target for neurological diseases.
- Other names
- HTR65-HT65-hydroxytryptamine receptor 65-HT6R
02
Mechanism of action
Agonists stimulate adenylate cyclase and increase intracellular cAMP levels. Antagonists increase acetylcholine/glutamate release in cortex/hippocampus while also facilitating dopamine/norepinephrine release in frontal cortex.
03
Biological functions
Signal transductionModulates cognitionModulates memoryModulates emotionModulates motor controlModulates neurotransmissionNeurodevelopment
04
Disease associations
Alzheimer’s diseaseParkinson’s diseaseSchizophreniaDepressionNeurodegenerative disease
05
Safety considerations
Potential for complex regulatory mechanisms leading to paradoxical effects (e.g., both agonists and antagonists showing procognitive and antidepressant/anxiolytic effects)Unknown long-term effects of chronic modulation of 5-HT6 receptor activity
06
Interacting drugs
5-HT6 receptor agonists
1 more in the full profile.
07
Biomarkers
C267T (rs1805054) polymorphism (Alzheimer's disease susceptibility)HTR6 gene variants (Parkinson's disease and other neuropsychiatric disorders)
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