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Azasetron hydrochloride

Y-25130 hydrochloride
A Potent Antagonist of Serotonin-Gated Channels
Cat #: Y-100
Alternative Name Y-25130 hydrochloride
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 386.3
    Purity: >98%
    Effective concentration 0.1-100 nM.
    Structure
    Chemical name N-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide;hydrochloride.
    Molecular formula C17H21Cl2N3O3.
    CAS No.: 123040-16-4.
    Activity Azasetron hydrochloride is a potent 5-HT3 channel blocker with a Ki ~2.9 nM1.
    References-Activity
    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 mM in H2O. 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 hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Azasetron hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Currents were elicited by 10 µM 5-HT delivered every 3 minutes. Azasetron hydrochloride (#Y-100) 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. Lee. H.Y. et al.  (2014) Cancer Res. Treat46, 19.
    2. Tsukagoshi, S. (1999) Gan To Kagaku Ryoho 26, 1001.
    3. Yun, M.J. et al. (2010) Yonsei Med. J. 51, 88.
    4. Yakushiji,T. and Akaike, N. (1992) Br. J. Pharmacol. 107, 853.
    5. Kato, S. et al. (2013) Biol. Pharm. Bull. 36,1406.
    Scientific background

    Azasetron hydrochloride (Y-25130 hydrochloride) is a potent 5-HT3 receptor antagonist. It selectively and competitively binds 5-HT3 receptors thereby blocking the serotonin binding site. Azasetron is classified as a derivative of benzamide. It has a different chemical structure from other 5-HT3 receptor blockers. The significant difference is found in the pharmacokinetic profiles resulting in a longer duration of action and a higher affinity for the 5-HT3 receptor1,2. Azasetron has an IC50 value ~4.9x10-10 M4 and half life of 5.4 hours3.

    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 mediate a variety of physiological functions5.

    Azasetron is mostly administered orally and by I.V (60-70%) and excreted in the urine in an unmetabolized form. Orally-administered azasetron is shown to be absorbed and secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability (approximately 90%)2.

    5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management and prevention of nausea and vomiting caused by cancer chemotherapy as well as postoperative nausea and emesis after anesthesia and surgery1,3.

    Target 5-HT3 receptors
    Last update: 23/08/2020

    Azasetron hydrochloride (#Y-100) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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