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 (55):

Cat. No. Product Name Effect Purity
  • HY-14541
    Olanzapine
    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
    Ondansetron
    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-U00121A
    Lintopride hydrochloride
    Antagonist
    Lintopride hydrochloride, a benzamide, is a potent 5HT-4 antagonist with moderate 5HT-3 antagonist properties. Lintopride hydrochloride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animal. Lintopride hydrochloride significantly increases the lower oesophageal sphincter (LOS) basal tone.
  • HY-106379
    Lurosetron
    Antagonist
    Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM..
  • 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
    Mirtazapine
    Antagonist 99.94%
    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-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-A0021
    Palonosetron hydrochloride
    Antagonist 99.96%
    Palonosetron hydrochloride is a 5-HT3 antagonist that inhibits chemotherapy-induced nausea and vomiting (CINV).
  • HY-15419
    RS-127445 hydrochloride
    Antagonist 99.78%
    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-B0002A
    Ondansetron hydrochloride dihydrate
    Antagonist 99.94%
    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-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-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-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-B0750
    Dolasetron
    Antagonist ≥98.0%
    Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
  • HY-B0020
    Tropisetron Hydrochloride
    Antagonist 99.97%
    Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.
  • HY-B0072
    Tropisetron
    Antagonist 98.72%
    Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 receptor antagonist (IC50: 70.1 nM) and α7-nicotinic receptor agonist.
  • HY-B0595
    Ramosetron Hydrochloride
    Antagonist 99.96%
    Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.
  • HY-B0071
    Granisetron
    Antagonist 99.95%
    Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  • HY-100552
    VUF10166
    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.