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Zacopride hydrochloride

A Potent Antagonist of 5-HT3 Receptors and an Agonist of 5-HT4 Receptors

Cat #: Z-110
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 346.25
    Purity: >98%
    Effective concentration 0.3-300 nM.
    Structure
    Chemical name 4-amino-N-(1-azabicyclo[2.2.2]octan-3-yl)-5-chloro-2-methoxybenzamide hydrochloride.
    Molecular formula C15H21Cl2N3O2.
    CAS No.: 99617-34-2
    Activity Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist (Ki = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM)1.
    References-Activity
    1. Cohen, M.L. et al. (1989) J. Pharmacol. Exp. Ther. 248, 197.
    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 Zacopride hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Zacopride hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Zacopride hydrochloride (#Z-110) 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. Bill, D.J. et al. (1995) Br. J. Pharmacol. 115, 775.
    2. Meyer, L.C. et al. (2006) Am. J. Physiol. 290, R405.
    3. Nagakura, Y. et al. (1999) Pharmacol. Res. 39, 375.
    Scientific background

    Zacopride hydrochloride is a derivative of benzamide, described as a potent 5-HT3 receptor antagonist with 5-HT4 receptor agonistic properties. Zacopride is a recemic compound. Studies showed that the S(-) form has a higher binding affinity for central and peripheral 5-HT3 receptor compared to R(+) zacopride1. Ki values for 5-HT3 and 5-HT4 receptors are 0.38 nM and 373 nM respectively3.

    There is some evidence from animal behavioral experiments that 5-HT3 receptor antagonists may be useful as anxiolytics, antipsychotics, cognition-enhancers and anti-addictive agents. It has been reported from these models that the S(-) enantiomer is potent in animal models of psychosis whereas the R(+) enantiomer is more potent in anxiety models1.

    Zacopride has been shown to be an effective anti-emetic agent against the emesis induced by cytotoxins and radiation in dogs, cats, non-human primates and ferrets2.

    Target 5-HT3, 5-HT4 receptors
    Lyophilized Powder
    Last update: 25/07/2021

    Zacopride hydrochloride (#Z-110) 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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