Serotonin 2A receptor, Serotonin 2B receptor, Serotonin 2C receptor (5-HT2A, 5-HT2B, 5-HT2C)

The serotonin 2A, 2B, and 2C receptors (5-HT2A, 5-HT2B, 5-HT2C) are closely related G protein-coupled receptors (GPCRs) that bind serotonin and mediate numerous central and peripheral physiological functions. The 5-HT2A receptor, present at high levels in the cortex and other brain regions, is critical for cognitive function, perception, and mood regulation and is the primary molecular target of psychedelic drugs. The 5-HT2C receptor is implicated in appetite, anxiety, and mood, and is a target for drugs intended to treat obesity and depression. The 5-HT2B receptor is expressed mainly in peripheral tissues, particularly the cardiovascular system, where its activation has been linked to cardiac valvulopathy. Collectively, drugs targeting these receptors are used or investigated for the treatment of psychiatric disorders (such as schizophrenia and depression), neurodegenerative disease, and metabolic disorders, but their modulation presents therapeutic challenges due to adverse effects such as hallucinations (especially with 5-HT2A agonists) and heart valve disease (with 5-HT2B agonists)[1][3][5][6][8].

Other names

5-hydroxytryptamine 2A receptor5-hydroxytryptamine 2B receptor5-hydroxytryptamine 2C receptorHTR2A, HTR2B, HTR2CSerotonin receptor 2A, 2B, 2C

Agonist binding (activates receptor signaling cascade leading to various CNS and peripheral effects). Antagonist/inverse agonist binding (blocks or reverses receptor activity, used in psychosis and depression). Functional selectivity/biased agonism (different drugs modulate distinct downstream pathways). Modulation of neurotransmitter release (notably dopamine and serotonin).