Overview
- Cohen, M.L. et al. (1989) J. Pharmacol. Exp. Ther. 248, 197.
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.
- Bill, D.J. et al. (1995) Br. J. Pharmacol. 115, 775.
- Meyer, L.C. et al. (2006) Am. J. Physiol. 290, R405.
- 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.
Zacopride hydrochloride (#Z-110) is a highly pure, synthetic, and biologically active compound.
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