Target intelligence / Profile preview

Serotonin 6 Receptor (5-HT6)

Target
5-HT6
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The serotonin 6 receptor (5-HT6) is a subtype of serotonin receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR), specifically coupled to the stimulatory Gs protein, and mediates excitatory neurotransmission by increasing intracellular cAMP levels through activation of adenylate cyclase. Its expression is almost exclusive to the brain, with key regions including the olfactory tubercle, cerebral cortex, nucleus accumbens, striatum, caudate nucleus, and hippocampus. This distribution suggests roles in motor control, emotionality, cognition, and memory. Preclinical studies support therapeutic potential for cognitive dysfunction associated with Alzheimer’s disease as well as for depression/anxiety. Some ligands targeting this receptor are under clinical development for anti-dementia or anti-obesity indications.

Other names
HTR65-HT6R5-hydroxytryptamine receptor 6
02

Mechanism of action

Gs protein activation, increased cAMP production

03

Biological functions

Signal transductionModulation of neuronal excitabilitySynaptic plasticityRegulation of cognitionRegulation of memory processesMood modulation
04

Disease associations

Alzheimer's diseaseDepressionAnxietyObesityNeurodegenerative disease
05

Interacting drugs

Atypical antipsychotics

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