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

5-HT3 Receptor

5-HT3 receptor is a serotonin-gated, cation-selective Cys-loop ligand-gated ion channel in the central and peripheral nervous systems[1]. Mechanistically, ligand binding triggers conformational changes around the orthosteric binding site and opens an intrinsic cation-selective channel that supports fast serotonergic neurotransmission[2]. Functional receptors require at least one 5-HT3A subunit, while 5-HT3B-5-HT3E subunits assemble with 5-HT3A and mainly modify receptor expression, conductance, or biophysical behavior[3]. Compared with other serotonin receptor families, 5-HT3 receptors are ion channels rather than G-protein-coupled receptors, which makes them distinct pharmacological and electrophysiological targets[4]. In disease-relevant research, selective 5-HT3 receptor antagonists are established for chemotherapy-induced and postoperative nausea and vomiting, and clinical use also includes irritable bowel syndrome[1][4]. In sensory models, rat dorsal root ganglion neurons express functional 5-HT3 receptors, and agonist-evoked Ca2+ influx can increase neurotransmitter release from DRG to spinal neurons[5]. For experimental applications, agonists, competitive antagonists, and allosteric modulators help define ligand binding, channel gating, and subunit-dependent receptor function[2][6].

5-HT3 Receptor Related Products (31):

Cat. No. Product Name Effect Purity
  • HY-15414
    Vortioxetine
    		Inhibitor 98.61%
    Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM).
  • HY-14564A
    GTS-21 dihydrochloride
    		Antagonist 99.65%
    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-15414A
    Vortioxetine hydrobromide
    		Inhibitor 99.87%
    Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-100938
    m-CPBG hydrochloride
    		Agonist 99.85%
    m-CPBG (1-(3-Chlorophenyl)biguanide) hydrochloride is a selective 5-HT3 agonist. m-CPBG hydrochloride can be used for the research of neurological disease.
  • HY-B0750
    Dolasetron
    		99.90%
    Dolasetron (MDL-73147) is a serotonin 5-HT3 receptor antagonist. Dolasetron acts as an antiemetics agent and can be used for the research of chemotherapy-induced nausea and vomiting in cancer.
  • HY-WAA0304
    Agmatine
    Agmatine is an orally active analgesic that can cross the blood-brain barrier. Agmatine targets the 5-HT2A receptor, 5-HT3 receptor, α2-adrenergic receptor, and I1 imidazoline receptor. Agmatine produces dose-dependent analgesic effects in various pain models. Agmatine can be used in research related to visceral pain, neuropathic pain, and inflammatory pain.
  • HY-185345
    GR119566X
    		Ligand
    GR119566X is a 5-HT3 receptor ligand with a pKi value of 8.80 against prufied 5-HT3 receptor. GR119566X can be used for 5-HT3 receptor purification.
  • HY-121001
    Amanozine
    		Agonist
    Amanozine (Compound 15) is a 5-HT3 serotonin receptor agonist. Amanozine is promising for research of nervous system disorders.
  • HY-75813
    2-Aminonicotinaldehyde
    		99.98%
    2-Aminonicotinaldehyde is a synthetic intermediate. 2-Aminonicotinaldehyde can be used for the synthesis of 5-HT3 receptor antagonists, AKT inhibitors, and other compounds. 2-Aminonicotinaldehyde is applicable to research on depression and cancers (including hepatocellular carcinoma).
  • HY-103118
    PU02
    		Antagonist 99.76%
    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.
  • HY-101046
    Quipazine dimaleate
    		Agonist 99.96%
    Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research.
  • HY-15414R
    Vortioxetine (Standard)
    		Inhibitor
    Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-101709
    Ricasetron
    		Antagonist 98.62%
    Ricasetron (BRL-46470) is a selective and orally active 5-HT3 receptor antagonist. Ricasetron displays little or no affinity for a variety of other neurotransmitter receptors. Ricasetron has anxiolytic and antiemetic effects.
  • HY-178907
    SERT/5-HT-IN-1
    		Inhibitor
    SERT/5-HT-IN-1 (compound D17) is an orally active and potent dual target inhibitor of SERT/5-HT3A (SERT IC50 = 1.5 nM, NET IC50 = 49 nM, DAT IC50 = 91 nM, 5-HT3A Ki = 12 nM). SERT/5-HT-IN-1 has an IC50 of 39 nM to 5-HT3A. SERT/5-HT-IN-1 has a lower risk of liver, kidney, and cardiac toxicity. SERT/5-HT-IN-1 can be used for research on depressive disorders.
  • 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.
  • HY-185345A
    GR119566X dihydrochloride
    		Ligand
    GR119566X dihydrochloride is a 5-HT3 receptor ligand with a pKi value of 8.80 against prufied 5-HT3 receptor. GR119566X dihydrochloride can be used for 5-HT3 receptor purification.
  • HY-15414AS
    Vortioxetine-d8 hydrobromide
    		Inhibitor 99.41%
    Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-105449A
    KB R6933
    		Antagonist
    KB R6933 (KB 6806 maleate) is a potent, selective and orally active 5-HT3 receptor antagonist. KB R6933 can inhibit the diarrhea induced by 5-HT (HY-B1473A), but not that by Castor Oil (HY-107799) or prostaglandin E2 (PGE2) (HY-101952). KB R6933 can inhibit 5-HT-induced bradycardia.
  • HY-182701
    5-HT3 antagonist-7
    		Antagonist
    5-HT3 antagonist-7 (Compound 7e) is a competitive and selective 5-HT3 receptor antagonist. 5-HT3 antagonist-7 inhibits 5-HT-induced contractions in guinea pig ileum and guinea pig thoracic aorta. 5-HT3 antagonist-7 prevents 2-methyl-5-HT-induced vomiting episodes in ferrets.
  • HY-15414S
    Vortioxetine-d8
    		Inhibitor
    Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).