5-HT3 receptor antagonists (setrons like ondansetron, granisetron) work by blocking serotonin receptors in the gut and CNS's chemoreceptor trigger zone. Their primary clinical use is as antiemetic agents for preventing and treating nausea and vomiting, especially chemotherapy-induced and post-operative nausea. They are not antidepressants, CNS stimulants, anxiolytics, or antiepileptics.