Serotonin receptor type 3 (5-HT₃ receptor)

Serotonin receptor type 3 (5-HT₃ receptor) is a member of the Cys-loop superfamily of ligand-gated ion channels and is structurally and functionally distinct from other serotonin (5-HT) receptors, which are G protein-coupled receptors[1][5][6][3]. The 5-HT₃ receptor forms a pentameric structure that acts as a cation-selective channel permeable to sodium, potassium, and calcium. It plays a pivotal role in fast excitatory neurotransmission in both the central and peripheral nervous systems and is highly expressed in areas related to emesis, including the brainstem and gastrointestinal tract[1][3][6][9]. Activation of the 5-HT₃ receptor by serotonin results in rapid neuronal depolarization, leading to effects such as vomiting, nausea, and modulation of gut motility. Clinically, pharmacological antagonists of the 5-HT₃ receptor are widely used to treat and prevent nausea and vomiting, particularly in the context of chemotherapy, radiotherapy, and postoperative recovery[7][9]. The receptor is also being studied in relation to additional CNS and gastrointestinal disorders.

Other names

5-hydroxytryptamine receptor 35-HT3 receptor5-HT3RSerotonin-gated ion channel

Antagonism (blockade) of serotonin binding at the 5-HT₃ receptor; Inhibition of ligand-gated cation channel opening