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

Target
5-HT2A (for Serotonin receptor 2A), 5-HT2C (for Serotonin receptor 2C)
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

Serotonin receptor 2A (5-HT2A) and serotonin receptor 2C (5-HT2C) are closely related G protein-coupled receptors (GPCRs) that mediate the actions of serotonin (5-hydroxytryptamine) in the central nervous system and peripheral tissues[1][2][10]. Both receptor subtypes are part of the 5-HT2 receptor family and primarily couple to Gq/11 proteins, resulting in increased intracellular inositol phosphate signaling[5][7]. 5-HT2A receptors are highly expressed in the cortex and play a key role in mood, cognition, and the actions of hallucinogenic drugs such as LSD and psilocybin[7][10]. They are prominent therapeutic targets in the treatment of neuropsychiatric disorders like schizophrenia, depression, and sleep disruptions[6][10]. 5-HT2C receptors are implicated in regulating appetite, mood, and addiction behaviors, making them targets for anti-obesity and anti-addiction drugs[3]. Both receptors are engaged by a broad array of pharmacological agents, including antipsychotics, antidepressants, and hallucinogens, and their complex signaling and pharmacology are the subject of ongoing therapeutic and mechanistic research[2][4][6]. If you need information on one specific subtype only (2A or 2C), each has distinct, but overlapping, functions and drug interactions. Both are valid, therapeutically relevant targets.

Other names
5-hydroxytryptamine receptor 2A5-hydroxytryptamine receptor 2CHTR2A (gene name for 2A)HTR2C (gene name for 2C)5-HT2A receptor5-HT2C receptor5HT2A5HT2C
02

Mechanism of action

- Agonism (e.g., hallucinogenic effect by psychedelic compounds through 5-HT2A activation) - Antagonism or inverse agonism (antipsychotic drugs, especially targeting 5-HT2A, block receptor signaling) - Modulation of downstream Gq/11-mediated phospholipase C signaling

03

Biological functions

Signal transductionRegulation of moodCognitionMemoryAppetite regulation (mainly 2C)Vascular tone regulation (mainly 2A)Modulation of hallucinations (mainly 2A)
04

Disease associations

Neuropsychiatric diseaseDepressionSchizophreniaAddiction/substance use disorderObesity (primarily 2C)
05

Safety considerations

Hallucinations and perceptual disturbances (primarily 5-HT2A agonism)Metabolic syndrome and weight gain (antipsychotics with 5-HT2C antagonism)Risk of serotonin syndrome with polypharmacyPotential for misuse/abuse (psychedelic compounds)
06

Interacting drugs

LSD (lysergic acid diethylamide)

11 more in the full profile.

07

Biomarkers

5-HT2A receptor density (PET imaging for psychiatric disorder studies)5-HT2C receptor RNA editing status (as a readout for certain neuropsychiatric states in research)

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