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VUF 10166

A Potent Antagonist of 5-Hydroxytryptamine Receptor 3A and 3B, and an Antagonist of H4 Histamine Receptor

Cat #: V-115
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 262.74
    Purity: >99%
    Effective concentration 0.05 nM – 100 nM.
    Structure
    Chemical name 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline.
    Molecular formula C13H15Cl2N4.
    CAS No.: 155584-74-0
    Activity VUF 10166 is a potent and selective 5-HT3A and B receptor antagonist1.
    References-Activity
    1. Thompson, A.J. et al. (2012) J. Pharmacol. Exp. Ther. 341, 350.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs VUF 10166 blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs VUF 10166 blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. VUF 10166 (#V-115) was applied 30 seconds before stimulation at 1 ,10 and 100 nM, as indicated and inhibited the 5-HT induced current in a dose-dependent and reversible manner.
    References - Scientific background
    1. Thompson, A.J. et al. (2014) Neuropharmacology 86, 378.
    2. Thompson, A.J. et al. (2012) J. Pharmacol. Exp. Ther. 341, 350.
    3. Thompson, A.J. et al. (2013) ChemMedChem 8, 946.
    4. Kato, S. et al. (2013) Biol. Pharm. Bull. 36, 1406.
    Scientific background

    VUF 10166 is a potent and selective antagonist of 5-HT3A and B receptors. It binds specifically and with high affinity to 5-HT3A (IC50 ~ 0.04 nM) and blocks the serotonin binding site. There's evidence of lower affinity to 5-HT3A/B receptors due to the influence of an additional allosteric binding site in the heteromer2.

    VUF 10166 is able to bind to an orthosteric binding site of HT3A and 5-HT3A/B receptors - A+A− and an A+B− interface. binding to the A+B− interface in the 5-HT3A/B receptor may decrease the affinity of ligands binding to the A+A− site by allosterically increasing the rate of ligand dissociation from the adjacent orthosteric site1,3.

    The 5-HT3 receptor subtype is a member of the Cys-loop ligand-gated cation channels which are expressed throughout the central and peripheral nervous systems and mediates a variety of physiological functions4.

    Competitive antagonists of 5-HT3 receptors are used to treat symptoms of emesis arising from chemotherapy treatment and postoperative emesis after anesthesia and surgery. There is also a limited use of antagonists for treating irritable bowel syndrome2.

    Target 5-Hydroxytryptamine Receptor 3A and 3B
    Lyophilized Powder
    Last update: 25/07/2021

    VUF 10166 (#V-115) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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