Serotonin 5-HT₂A receptor (5-HT₂A receptor)

The **Serotonin 5-HT₂A receptor** is a member of the class A GPCR family, activated primarily by serotonin (5-hydroxytryptamine). It is widely expressed in the central nervous system—especially in the cortex and hippocampus—as well as peripherally in platelets, vasculature, and various organs[3][6][1]. The receptor mediates signal transduction via Gq/11 proteins, leading to phospholipase C activation and intracellular calcium mobilization[7]. It regulates key functions such as mood, cognition, sleep, behavior, platelet aggregation, and cardiovascular processes, and plays a vital role in the mechanisms of psychedelic drug action, antipsychotic therapy, and the modulation of cardio- and cerebrovascular platelets[2][3][4][5][6][7]. Dysregulation of 5-HT₂A receptor activity is implicated in major psychiatric disorders, while targeted drugs include both agonists (producing psychedelic effects) and antagonists (used for psychosis, depression, and other indications). Safety and efficacy are challenged by broad pharmacology and side-effect profiles, necessitating selective ligand development.

Other names

5-hydroxytryptamine receptor 2A5-HT2A5HT2AHTR2A

**Agonism:** Activation leads to Gq/11-coupled intracellular signaling, increased PLC activity, and psychedelic-like effects[4][7]. **Antagonism:** Blockade prevents serotonin-mediated neurotransmission and modulates dopamine, used in antipsychotic and antidepressant therapy[5][6][2]. **Functional selectivity (bias):** Ligands can differentially activate Gq/11 (classical signaling) or β-arrestin2 pathways, resulting in distinct therapeutic or psychedelic profiles[4][7].