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The 5-HT3 receptor is a ligand-gated ion channel that mediates fast excitatory neurotransmission in both the central and peripheral nervous systems. It is activated by serotonin and plays a role in various physiological processes including emesis, pain perception, anxiety, and gut motility. The receptor is a pentameric structure, primarily composed of 5-HT3A subunits, but can also form heteromers with 5-HT3B, 5-HT3C, 5-HT3D, and 5-HT3E subunits. Drugs targeting the 5-HT3 receptor, such as the "setrons", are commonly used as antiemetics.
Activation of the receptor by serotonin opens the cation-selective channel allowing Na+ and K+ influx, leading to neuronal depolarization and excitation.
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