5-HT3 Selective Inhibitors | Agonists | Antagonists | Modulators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S5052 Granisetron

Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.

Selective
S4694 Alosetron Hydrochloride

Alosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

Selective
S2865 VUF 10166

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

Selective 5-HT3AB, Ki: 22 nM; 5-HT3A, Ki: 0.04 nM
S3723 Ramosetron Hydrochloride

Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.

Selective 5-HT3 receptor, Ki: 0.091 nM
S5740 Palonosetron

Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

Selective 5-HT3 receptor, Ki: 0.17 nM
S2106 Azasetron HCl

Azasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

Selective 5-HT3, IC50: 0.33 nM
S5538 Tropisetron

Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

Selective 5-HT3 receptor, Ki: 5.3 nM
S4748 Ondansetron Hydrochloride Dihydrate

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

Selective 5-HT3 receptor, IC50: 810 nM
S2644 Lerisetron

Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM.

Selective 5-HT3 receptor, IC50: 0.81 μM
S2578 1-Phenylbiguanide

1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.

Selective 5-HT3 receptor, EC50: 3.0 μM
S1390 Ondansetron HCl

Ondansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.

Selective
S1345 Granisetron HCl

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.

Selective
S2464 Sevoflurane

Sevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.

Selective
S1996 Ondansetron

Ondansetron (GR 38032F, GR-C507/75) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

Selective
S1898 Tropisetron HCl

Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

Selective
S3050 Palonosetron HCl

Palonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.

Selective
S8021 Vortioxetine (Lu AA21004) HBr

Vortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM.

Pan 5-HT3A, Ki: 3.7 nM