Zacopride (hydrochloride)

Zacopride hydrochloride is an orally active 5-HT₃ receptor (K_i of 0.38 nM) antagonist and 5-HT₄ receptor (K_i of 373 nM) agonist. Zacopride hydrochloride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride hydrochloride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety^{[1][2][3][4][5][6][7][8][9][10][11]}. In Vitro:Zacopride (3-30 μM) hydrochloride reduces the 5-HT-induced maximum contraction response of guinea pig colon in a concentration-dependent manner^[3].
Zacopride hydrochloride produces 5-HT₄ receptor-mediated relaxation of the rat esophagus with an EC₅₀ value of 0.5 μM^[3].
Zacopride hydrochloride (10 μM) shortens duration of action potentials in guinea pig isolated papillary muscles^[11].
In Vivo:Zacopride (0.1 mg/kg; p.o.; single dose) hydrochloride can induce vomiting in ferrets^[4].
Zacopride (0.1 mg/kg; intraperitoneal injection; single dose) hydrochloride can completely block the vomiting induced by oral administration of 0.1 mg/kg Zacopride in ferrets^[4].
Zacopride hydrochloride (0.1 mg/kg; intraperitoneal injection; single dose) hydrochloride can significantly attenuate the increase in extracellular dopamine levels in the nucleus accumbens induced by cocaine in rats^[5].
Zacopride (Zacopride chlorhydrate, 1.0 mg/kg; intraperitoneal injection; single dose) hydrochloride combined with Tacrine can improve the accuracy of rats at the shortest delay (0-4 s) in a spatial working memory task^[6].
Zacopride hydrochloride (0.01-31.6 mg/kg; p.o.; multiple doses until vomiting occurs) induces vomiting in 100% of ferrets at a cumulative dose of 0.11 mg/kg^[7].
Zacopride hydrochloride (0.5 mg/kg; intravenous injection; single dose) combined with Etorphine can alleviate the decrease in respiratory rate caused by Etorphine in goats, increase hemoglobin oxygen saturation and arterial oxygen tension, while reducing carbon dioxide tension and improving ventilation^[8].
Zacopride (0.1-1.0 mg/kg; intraperitoneal injection; single dose) hydrochloride exhibits anxiolytic effects in mice (social interaction and elevated plus maze test)^[9].
Zacopride (0.0001-10 mg/kg; intraperitoneal injection; single dose) hydrochloride can enhance the exploratory behavior (black-white test box test) and social interaction (social interaction test with rats) of mice^[10].