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Lerisetron

A Potent Antagonist of 5-HT3 Channels

Cat #: L-175
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 292.4
    Purity: >98%
    Effective concentration 0.5-100 nM.
    Structure
    Chemical name 1-benzyl-2-piperazin-1-ylbenzimidazole.
    Molecular formula C18H20N4.
    CAS No.: 143257-98-1
    PubChem CID 65997
    Activity Lerisetron inhibits the 5-HT-induced Bezold-Jarisch reflex in anesthetized rats, pKi = 9.21.
    References-Activity
    1. Orjales, A. et al. (1997) J. Med. Chem. 40, 586.
    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 Lerisetron blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Lerisetron blocks 5-HT3A receptors expressed in HEK 293T cells. 
      5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Lerisetron (#L-175) 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. Gomez-de-Segura, I.A. et al. (1998Acta. Oncol. 37, 759.
    2. Jauregizar, N. et al. (2002) J. Pharm. Sci. 91, 41.
    3. Ortega, F. et al. (2005) Pharm. Res. 22, 1769.
    4. Kato, S. (2013Biol. Pharm. Bull. 36, 1406.
    Scientific background

    Lerisetron, a piperazinylbenzimidazole derivative, is a potent and highly selective blocker of serotonin 5-HT3 channels with antiemetic effects. The drug is shown to be effective in the treatment of nausea and vomiting caused by emetogenic cytotoxic drugs1,2.

    Lerisetron antagonizes the serotonin action on the presynaptic 5-HT3 receptor that is implicated at the emetic reflex2,3.

    The 5-HT3 receptor mediates the action of serotonin in the body. This receptor 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 functions such as: emotion, cognition, memory, pain perception, and gastrointestinal functions including secretion and motility4.

    Target 5-HT3A receptors
    Last update: 24/01/2021

    Lerisetron (#L-175) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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