Zacopride 

Zacopride 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 exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride 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]}.

Zacopride (3-30 μM) reduces the 5-HT-induced maximum contraction response of guinea pig colon in a concentration-dependent mannersup^[3].
Zacopride produces 5-HT₄ receptor-mediated relaxation of the rat esophagus with an EC₅₀ value of 0.5 μM^[3].
Zacopride (10 μM) shortens duration of action potentials in guinea pig isolated papillary muscles^[11].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zacopride (0.1 mg/kg; p.o.; single dose) can induce vomiting in ferrets^[4].
Zacopride (0.1 mg/kg; intraperitoneal injection; single dose) can completely block the vomiting induced by oral administration of 0.1 mg/kg Zacopride in ferrets^[4].
Zacopride (0.1 mg/kg; intraperitoneal injection; single dose) 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) combined with Tacrine can improve the accuracy of rats at the shortest delay (0-4 s) in a spatial working memory task^[6].
Zacopride (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 (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) exhibits anxiolytic effects in mice (social interaction and elevated plus maze test)^[9].
Zacopride (0.0001-10 mg/kg; intraperitoneal injection; single dose) can enhance the exploratory behavior (black-white test box test) and social interaction (social interaction test with rats) of mice^[10].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

309.79

C₁₅H₂₀ClN₃O₂

90182-92-6

O=C(C1=C(OC)C=C(N)C(Cl)=C1)NC2CN3CCC2CC3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Neumann J, et al. Zacopride stimulates 5-HT4 serotonin receptors in the human atrium. Naunyn Schmiedebergs Arch Pharmacol. 2024 Sep;397(9):6821-6835.  [Content Brief]

  [2]. Pinkus L M, et al. Utilization of Zacopride and its R-and S-Enantiomers in Studies of 5-HT 3 Receptor “Subtypes”. Serotonin: Molecular Biology, Receptors and Functional Effects, 1991: 439-448.

  [3]. Nagakura Y, et al. Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacol Res. 1999 May;39(5):375-82.  [Content Brief]

  [4]. Sancilio LF, et al. Emetic activity of zacopride in ferrets and its antagonism by pharmacological agents. Eur J Pharmacol. 1990 Jun 8;181(3):303-6.  [Content Brief]

  [5]. McNeish CS, et al. The 5-HT3 antagonist zacopride attenuates cocaine-induced increases in extracellular dopamine in rat nucleus accumbens. Pharmacol Biochem Behav. 1993 Aug;45(4):759-63.  [Content Brief]

  [6]. Jäkälä P, et al. The effects of tacrine and zacopride on the performance of adult rats in the working memory task. Gen Pharmacol. 1993 May;24(3):675-9.  [Content Brief]

  [7]. Sancilio LF, et al. Studies on the emetic and antiemetic properties of zacopride and its enantiomers. Eur J Pharmacol. 1991 Jan 17;192(3):365-9.  [Content Brief]

  [8]. Meyer LC, et al. Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats. Am J Physiol Regul Integr Comp Physiol. 2006 Feb;290(2):R405-13.  [Content Brief]

  [9]. Dunn R W, et al. Preclinical anxiolytic versus antipsychotic profiles of the 5‐HT3 antagonists ondansetron, zacopride, 3α‐tropanyl‐1H‐indole‐3‐carboxylic acid ester, and 1αH, 3α, 5αH‐tropan‐3‐yl‐3, 5‐dichlorobenzoate. Drug development research, 1991, 23(4): 289-300.

  [10]. Costall B, et al. Zacopride: anxiolytic profile in rodent and primate models of anxiety. J Pharm Pharmacol. 1988 Apr;40(4):302-5.  [Content Brief]

  [11]. Kii Y, et al. Effects of 5-HT4-receptor agonists, cisapride, mosapride citrate, and zacopride, on cardiac action potentials in guinea pig isolated papillary muscles. J Cardiovasc Pharmacol. 1997 May;29(5):670-5.  [Content Brief]