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The serotonin 5-HT3 receptor is a ligand-gated ion channel that mediates fast excitatory neurotransmission in both the central and peripheral nervous systems. Upon binding serotonin, the channel opens, allowing the influx of cations like Na+, K+, and Ca2+, leading to neuronal depolarization. Antagonists of this receptor are clinically used as antiemetics and in the treatment of irritable bowel syndrome. The receptor is a pentamer composed of subunits including 5-HT3A, 5-HT3B, HTR3C, HTR3D, and HTR3E, which can form homo- or heteromeric channels. Genetic polymorphisms in the genes encoding these subunits can affect receptor expression and function.
Antagonists bind to the receptor, blocking serotonin binding and preventing channel opening.
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