Ramosetron HCl is a potent and selective 5-HT3 receptor antagonist for the treatment of nausea and vomiting.

Ondansetron HCl 2H2O is a competitive 5-HT3 receptor antagonist.

VUF10166 is a potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.

Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

Alosetron HCl is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.

Azasetron HCl is a potent, selective and competitive 5-HT3 receptor antagonist with pKi value of 9.27.

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.

Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).