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The 5-hydroxytryptamine receptor 3 (5-HT₃ receptor) is a ligand-gated ion channel that mediates fast excitatory neurotransmission in both the central and peripheral nervous systems. Upon activation by serotonin, the channel opens to allow Na⁺, K⁺, and Ca²⁺ ions through, resulting in rapid neuronal depolarization and excitation. It plays roles in emesis, cognition, anxiety, gastrointestinal motility, and neurodevelopment. Antagonists like ondansetron are used clinically to prevent nausea/vomiting.
Selective antagonists block the receptor's action within brainstem emetic centers, preventing nausea/vomiting.
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