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Target intelligence / Profile preview
5-hydroxytryptamine 6 receptor
- Molecular classification
- GPCR, G protein-coupled receptor, Rhodopsin family receptor
01
Overview
The 5-hydroxytryptamine 6 receptor (5-HT6 receptor, HTR6) is a G protein-coupled receptor (GPCR) for serotonin (5-hydroxytryptamine). It is almost exclusively expressed in the brain, with high abundance in regions associated with cognition and memory. Activation enhances cAMP signaling and modulates neurotransmission. It has been investigated as a therapeutic target for Alzheimer’s disease, schizophrenia, and obesity, but clinical trial results have been mixed.
02
Mechanism of action
Activation of adenylyl cyclase leading to increased cAMP formation; Modulation of neurotransmitter release (glutamate, acetylcholine, dopamine, norepinephrine, GABA); Regulation of CDK5 and mTOR signaling.
03
Biological functions
Signal transductionModulates neurotransmissionRegulates neuron migrationCorticogenesiscAMP signaling
04
Disease associations
Alzheimer's diseaseSchizophreniaObesityDepressionOCDAnxiety
05
Safety considerations
Clinical trial results have been mixed or negative for dementia-related indications despite promising preclinical data.Challenges in clinical translation despite robust preclinical rationale.
06
Interacting drugs
Tricyclic psychotropic drugs
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