1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT3 Receptor Isoform
  5. 5-HT3 Receptor Antagonist

5-HT3 Receptor Antagonist

5-HT3 Receptor Antagonists (51):

Cat. No. Product Name Effect Purity
  • HY-14541
    Antagonist 99.83%
    Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
  • HY-14564A
    GTS-21 dihydrochloride
    Antagonist 99.92%
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
  • HY-B0002B
    Antagonist 99.46%
    Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist, with IC50 value of 103 pM. Ondansetron exerts antiemetic effects by antagonizing 5-HT receptor located on local neurons in the peripheral and central nervous system. Ondansetron suppresses nausea and vomiting caused by chemotherapy and radiation therapy. Ondansetron has orally bioactivity.
  • HY-103152
    GR 113808
    Antagonist 99.96%
    GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
  • HY-B0352
    Antagonist 99.08%
    Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
  • HY-15419
    RS-127445 hydrochloride
    Antagonist 99.62%
    RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
  • HY-A0021
    Palonosetron hydrochloride
    Antagonist 99.96%
    Palonosetron hydrochloride is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
  • HY-B0071A
    Granisetron Hydrochloride
    Antagonist 99.90%
    Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  • HY-B0002A
    Ondansetron hydrochloride dihydrate
    Antagonist 99.03%
    Ondansetron (GR 38032) hydrochloride dehydrate is an orally active, highly selective and competitive 5-HT3 receptor antagonist (crosses the blood-brain barrier). Ondansetron hydrochloride dehydrate can be used in studies of preventing nausea and vomiting associated with cancer chemotherapy, radiation therapy and surgery.
  • HY-70050C
    Alosetron Hydrochloride
    Antagonist 99.76%
    Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
  • HY-32329A
    Setiptiline maleate
    Antagonist 99.94%
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
  • HY-B0020
    Tropisetron Hydrochloride
    Antagonist 99.90%
    Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.
  • HY-B0072
    Antagonist 98.72%
    Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.
  • HY-B0750
    Antagonist ≥98.0%
    Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
  • HY-A0008
    Talipexole dihydrochloride
    Antagonist 99.80%
    Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
  • HY-B0068
    Azasetron hydrochloride
    Antagonist 99.78%
    Azasetron (Y-25130) hydrochloride, a benzamide derivative, is a potent and selective 5-HT3 receptor antagonist. Azasetron is used in the study for Chemotherapy-induced nausea and vomiting (CINV).
  • HY-B1541
    Antagonist ≥99.0%
    Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Neuroprotective effect.
  • HY-100552
    Antagonist 99.83%
    VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM.
  • HY-B0595
    Ramosetron Hydrochloride
    Antagonist 99.95%
    Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.
  • HY-103118
    Antagonist ≥99.0%
    PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.