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

The serotonin 5-hydroxytryptamine 2A and 2C receptors are closely related G protein-coupled receptors (GPCRs) that mediate many of the effects of the neurotransmitter serotonin (5-HT) in the central nervous system and peripheral tissues[1][2][3][4]. The 5-HT2A receptor is especially abundant in the cortex and is the principal pharmacological target for many psychedelic drugs (such as LSD, psilocybin, and mescaline) as well as atypical antipsychotics (as an antagonist or inverse agonist)[1][6]. The 5-HT2C receptor shares similar signaling pathways, contributing to mood regulation, appetite, and neuroendocrine function. Activation of these receptors triggers the Gq/PLC pathway leading to increased intracellular calcium levels, and both receptor types are implicated in neuropsychiatric and neurodegenerative diseases[2][4][6]. Drugs targeting these receptors can act as agonists, antagonists, or inverse agonists, with therapeutic roles in depression, schizophrenia, and other disorders, but safety concerns include hallucinations, cardiovascular effects, and potential for abuse[4][6].

Other names

5-HT2A receptor5-HT2C receptor5-HT2A/C receptor5-hydroxytryptamine receptor 2A5-hydroxytryptamine receptor 2CSerotonin receptor 2ASerotonin receptor 2C

Agonist: stimulates receptor to activate Gq/PLC pathway, intracellular IP₃/DAG formation, and downstream PKC activation, leading to increases in intracellular calcium[5][1][3]. Antagonist: blocks receptor signaling, inhibits physiological and behavioral responses to serotonin or hallucinogens[3][4][6]. Inverse agonist: suppresses constitutive receptor activity[4].