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A Potent and Selective Antagonist of 5-HT3 Channels

Cat #: A-240
Alternative Name Y-25130
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 349.8
    Purity: >98%
    Effective concentration 0.1-100 nM.
    Chemical name N-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide.
    Molecular formula C17H20ClN3O3.
    CAS No.: 123040-93-7
    Activity Azasetron is a potent and selective 5-HT3 channel blocker with Ki ~2.9 nM1.
    1. Fukuda, T. et al. (1991) Eur. J. Pharmacol. 196, 299.
    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 100-150 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 Azasetron blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Azasetron blocks 5-HT3A receptors expressed in HEK 293T cells. 
      5-HT3A receptor currents were elicited with 10 µM 5-HT delivered every 3 minutes. Azasetron (#A-240) was applied 30 seconds before stimulation at 0.5, 1 and 20 nM, as indicated, and inhibited the 5-HT-induced current in a dose-dependent and reversible manner.
    References - Scientific background
    1. Yun, M.J. et al. (2010) Yonsei. Med. J. 51, 88.
    2. Lee, H.Y. et al. (2014) Cancer Res. Treat. 46, 19.
    3. Niwa, T. et al. (2006) Biol. Pharm. Bull. 29, 1931.
    4. Kato, S. et al. (2013) Biol. Pharm. Bull. 36, 1406.
    Scientific background

    Azasetron is a potent and selective 5-HT3 receptor antagonist. It antagonizes the channel by binding to 5-HT3 receptors thereby blocking the serotonin binding site and antagonizing the indirect sympathomimetic responses to 5-HT3.

    The compound is classified as a derivative of benzamide with a longer duration of action and higher affinity than other 5-HT3 receptor antagonists.

    Azasetron is highly effective in preventing postoperative and chemotherapy-induced nausea and vomiting induced by anticancer drugs and radiotherapy1,2. Therefore, in most cases 5-HT3 receptor antagonists are co-administered with anticancer drugs3.

    The 5-HT3 receptor subtype is a member of the cys-loop ligand-gated cation channels expressed throughout the central and peripheral nervous systems and mediate a variety of important physiological functions4.

    Target 5-HT3A, 5-HT3B
    Last update: 06/11/2022

    Azasetron (#A-240) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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