Target intelligence / Profile preview

Serotonin Receptor 5-HT2A (5-HT2A)

Target
5-HT2A
Molecular classification
G protein-coupled receptor (GPCR), Serotonin receptor
01

Overview

The serotonin 2A receptor (5-HT2A) is a G protein-coupled receptor that mediates excitatory neurotransmission in the central nervous system. It is involved in various physiological functions, including learning, memory, mood regulation, and perception. The receptor is implicated in psychiatric disorders such as depression and schizophrenia and is a target for psychedelic drugs, antipsychotics, and antidepressants. Activation by agonists leads to increased intracellular calcium and PKC activation, while antagonists block the receptor and prevent serotonin binding.

Other names
Serotonin 2A receptor5-hydroxytryptamine receptor 2AHTR2A
02

Mechanism of action

Agonists (e.g., LSD, psilocybin) activate the receptor, leading to increased intracellular calcium and PKC activation. Antagonists (e.g., atypical antipsychotics) block the receptor, preventing serotonin binding and downstream signaling.

03

Biological functions

NeurotransmissionSignal transductionVasoconstrictionPlatelet aggregationModulation of perception and cognitionRegulation of moodSynaptic plasticity
04

Disease associations

DepressionSchizophreniaDrug addiction
05

Safety considerations

Hallucinogenic effects of agonistsSide effects of antipsychotics (e.g., metabolic syndrome, extrapyramidal symptoms)Potential for receptor downregulation with chronic antidepressant use
06

Interacting drugs

LSD

3 more in the full profile.

07

Biomarkers

5-HT2A receptor density (in depression)

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