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Target intelligence / Profile preview
5-hydroxytryptamine 2A receptor (5-HT2A receptor)
- Target
- 5-HT2A receptor
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The 5-hydroxytryptamine 2A receptor (5-HT2A receptor) is a subtype of serotonin receptors, part of the G protein-coupled receptor family. It is highly expressed in the central nervous system, particularly in the prefrontal cortex, and also found in peripheral tissues like platelets and endothelial cells. It plays a role in cognition, perception, psychiatric disorders, and cardiovascular function. It is a target for psychedelic drugs and antipsychotics.
- Other names
- Serotonin receptor 2A5-HT2ARHTR2A
02
Mechanism of action
Agonist: Stimulation of phospholipase C (PLC), leading to production of inositol triphosphate (IP3) and diacylglycerol (DAG), release of calcium from intracellular stores, and activation of protein kinase C (PKC). Antagonist: Blocks the binding of serotonin and other agonists, preventing receptor activation.
03
Biological functions
Signal transductionNeuromodulationRegulation of vascular tonePlatelet functionModulation of learning and memoryNeurogenesis
04
Disease associations
DepressionSchizophreniaPsychiatric disordersCardiovascular disease
05
Safety considerations
Hallucinations (with agonists)Side effects associated with antipsychotics
06
Interacting drugs
Serotonin
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