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) 以浓度依赖的方式降低 5-HT 诱导的豚鼠结肠最大收缩反应^[3]。
Zacopride 可产生 5-HT₄ 受体介导的大鼠食管舒张反应，EC₅₀ 值为 0.5 μM^[3]。
Zacopride (10 μM) 可缩短豚鼠离体乳头肌动作电位的持续时间^[11]。

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

Zacopride (0.1 mg/kg；口服；单次给药) 可诱导雪貂呕吐^[4]。
Zacopride (0.1 mg/kg；腹腔注射；单次给药) 可完全阻断口服 0.1 mg/kg Zacopride 诱导的雪貂呕吐^[4]。
Zacopride (0.1 mg/kg；腹腔注射；单次给药) 可显著减弱 Cocaine 诱导的大鼠伏隔核细胞外多巴胺水平的升高^[5]。
Zacopride (Zacopride chlorhydrate, 1.0 mg/kg；腹腔注射；单次给药) 与 Tacrine 联合使用，可提高大鼠在空间工作记忆任务中最短延迟 (0-4 s) 时的正确率^[6]。
Zacopride (0.01-31.6 mg/kg；口服；多次给药直至呕吐发生) 在累积剂量为 0.11 mg/kg 时，诱使 100% 的雪貂发生呕吐^[7]。
Zacopride (0.5 mg/kg；静脉注射；单次给药) 与 Etorphine 联合使用，可减轻 Etorphine引起的山羊呼吸频率下降、提高血红蛋白氧饱和度和动脉血氧分压，同时降低二氧化碳分压，改善通气^[8]。
Zacopride (0.1-1.0 mg/kg；腹腔注射；单次给药) 在小鼠中表现出抗焦虑作用 (社交互动和高架十字迷宫实验)^[9]。
Zacopride (0.0001-10 mg/kg；腹腔注射；单次给药) 可增强小鼠探索行为 (黑白测试箱实验) 和社交互动 (与大鼠社交互动实验)^[10]。

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

309.79

C₁₅H₂₀ClN₃O₂

90182-92-6

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]