zacopride
Sign in to saveAlso known as AHR-11190-B, iodozacopride
Zacopride is a potent antagonist at the 5-HT3 receptor and an agonist at the 5-HT4 receptor. It has anxiolytic and nootropic effects in animal models, with the (R)-(+)-enantiomer being the more active form. It also has antiemetic and pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Early animal trials have also revealed that administration of zacopride can reduce preference for and consumption of ethanol.
Research
324 papers- Zacopride stimulates 5-HT(4) serotonin receptors in the human atrium.Naunyn-Schmiedeberg's archives of pharmacology · 2024
- Zacopride Exerts an Antiarrhythmic Effect by Specifically Stimulating the Cardiac Inward Rectifier Potassium Current in Rabbits: Exploration of a New Antiarrhythmic Strategy.Current pharmaceutical design · 2020
- Zacopride and BRL 24924 induce an increase in EEG-energy in rats.British journal of pharmacology · 1990
- The enantiomers of zacopride: an intra-species comparison of their potencies in functional and anxiolytic models.British journal of pharmacology · 1995
- Zacopride selectively activates the Kir2.1 channel via a PKA signaling pathway in rat cardiomyocytes.Science China. Life sciences · 2013
via PubMed
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Encyclopedic overview
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Zacopride is a potent antagonist at the 5-HT3 receptor and an agonist at the 5-HT4 receptor. It has anxiolytic and nootropic effects in animal models, with the (R)-(+)-enantiomer being the more active form. It also has antiemetic and pro-respiratory effects, both reducing sleep apnea and reversing opioid-induced respiratory depression in animal studies. Early animal trials have also revealed that administration of zacopride can reduce preference for and consumption of ethanol.
Zacopride was found to significantly increase aldosterone levels in human subjects for 180 minutes at a dose of 400 micrograms. It is thought to do this by stimulating the 5-HT4 receptors on the adrenal glands. Zacopride also stimulated aldosterone secretion when applied to human adrenal glands in vitro. No significant changes were observed in renin, ACTH, or cortisol levels.
Excerpted from Wikipedia’s “zacopride” article, available under the CC BY-SA 4.0 licence.