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Target intelligence / Profile preview
Serotonin 5‑HT₂A Receptor (5-HT2A)
- Target
- 5-HT2A
- Molecular classification
- G protein-coupled receptor, GPCR, Class A GPCR, Receptor
01
Overview
The serotonin 5‑HT₂A receptor (5-HT2A) is a G protein-coupled receptor that primarily couples to Gq/11 proteins, leading to activation of intracellular signaling cascades. It is highly expressed in the central nervous system, especially the frontal cortex, and is involved in cognition, memory formation, and mood regulation. Peripherally, it mediates vasoconstriction and platelet aggregation. Psychedelic drugs such as LSD and psilocybin are potent agonists, while many atypical antipsychotics act as antagonists. Overexpression or abnormal activity is linked with depression and schizophrenia. Activation by psychedelics promotes neuroplasticity.
- Other names
- 5-Hydroxytryptamine receptor 2ASerotonin receptor 2A
02
Mechanism of action
Agonism (e.g., LSD, psilocybin); Antagonism (e.g., atypical antipsychotics); Modulation of dopamine release; Activation of PLC/IP₃/DAG/Ca²⁺ pathway
03
Biological functions
Signal transductionLearningMemory formationNeurogenesisSpatial cognitionMood regulationVasoconstrictionPlatelet aggregationNeuroplasticity
04
Disease associations
DepressionSchizophreniaPsychosisAddictionPsychiatric disorders
05
Safety considerations
Hallucinogenic effects (agonists)Extrapyramidal side effects (typical antipsychotics, less so with atypicals targeting 5-HT2A)
06
Interacting drugs
LSD
3 more in the full profile.
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