Target intelligence / Profile preview

Serotonin receptor 2A and Serotonin receptor 2C (5-HT2A, 5-HT2C)

Target
5-HT2A, 5-HT2C
Molecular classification
G protein-coupled receptor (GPCR), Receptor, 7-transmembrane receptor
01

Overview

Serotonin receptor 2A (5-HT2A) and Serotonin receptor 2C (5-HT2C) are closely related G protein-coupled receptors that mediate the actions of serotonin in the central nervous system and peripheral tissues.[2][3] 5-HT2A is a principal target for psychedelic drugs and many antipsychotics, and plays a major role in mood, cognition, and perception[3][5]. 5-HT2C is central to appetite regulation and is a therapeutic target for anti-obesity drugs, as well as being implicated in mood and endocrine regulation[2][6]. These receptors can form functional complexes (heterodimers), and both are implicated in psychiatric, metabolic, and cognitive disorders, making them significant in neuropharmacology and therapeutics[7][9].

Other names
5-HT2A receptor5-HT2C receptorHTR2A (gene, for 2A)HTR2C (gene, for 2C)Serotonin 2A receptorSerotonin 2C receptor
02

Mechanism of action

Agonists activate Gq/11 protein signaling, increase IP3/DAG, elevate intracellular calcium, modulate neurotransmission\nAntagonists block activation, reducing downstream effects\nSome ligands (e.g., LSD) trigger β-arrestin recruitment (biased agonism)\n5-HT2A/2C heterodimer interactions can modulate receptor function

03

Biological functions

Signal transductionModulation of neurotransmissionRegulation of mood, perception, cognition (especially 2A)Regulation of appetite, endocrine secretion (especially 2C)Control of sleep, memory, learning
04

Disease associations

Neuropsychiatric disorders (depression, schizophrenia, anxiety, psychosis, addiction)Obesity and metabolic disorders (mainly 2C)Mood disordersCognitive disordersPotential role in neurodegeneration
05

Safety considerations

5-HT2A: Hallucinations, psychosis with agonists; side effects with antagonists5-HT2C: Appetite suppression, mood alterations; effect on other neurotransmitter systemsDrug interactions and off-target effects, such as serotonin syndrome or metabolic syndrome with antipsychotics
06

Interacting drugs

Agonists/antagonists: LSD, psilocybin, MDMA, DOI, mescaline (psychedelics—mainly 2A)

4 more in the full profile.

07

Biomarkers

HTR2A and HTR2C gene polymorphisms as genetic biomarkers in psychiatric and metabolic disorders (e.g. response to antipsychotics, obesity risk)Receptor binding density (PET imaging research)

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