Zacopride hydrochloride

A Potent Antagonist of 5-HT3 Receptors and an Agonist of 5-HT4 Receptors
    Cat #: Z-110
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 346.25
    Purity: >98%
    Effective concentration 0.3-300 nM.
      • Zacopride hydrochloride
    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, 101303-98-4.
    Activity Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist (Ki = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM)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.
      • Zacopride hydrochloride
        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.
      • 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
    Last update: 24/01/2020

    Zacopride hydrochloride (#Z-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
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