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Zacopride hydrochloride

产品编号 T5336 CAS 101303-98-4

Zacopride hydrochloride 是5-HT3受体拮抗剂 (Ki:0.38 nM)，也是5-HT4受体激动剂 (Ki:373 nM)，具有抗焦虑作用。它对精神分裂症具有潜在的研究价值。

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Zacopride hydrochloride Chemical Structure

Zacopride hydrochloride, CAS 101303-98-4

规格	价格/CNY	货期
1 mg	￥ 379	现货
5 mg	￥ 898	现货
10 mg	￥ 1,490	现货
25 mg	￥ 2,990	现货
50 mg	￥ 4,390	现货
100 mg	￥ 6,290	现货
1 mL * 10 mM (in DMSO)	￥ 987	现货

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其他形式的 Zacopride hydrochloride:

Zacopride
询价

选择批次

纯度: 98.32%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Zacopride is a highly potent 5-HT3 receptor antagonist (Kd = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM). It also is a selective IK1 channel agonist.
靶点活性	5-HT4:373 nM (Ki, cell free), 5-HT3:0.38 nM (Kd, cell free)
体外活性	Zacopride (0.1-10 μmole/L) dose-dependently enhanced the IK1 current in isolated rat cardiomyocytes, had no effects on other ion channels, transporters, or pumps [2]. In Langendorff perfused rat hearts, the antiarrhythmic effect of 1 μmol/L zacopride were reversed by 1 μmol/L BaCl2, a blocker of IK1 channel. In Kir2.x transfected Chinese hamster ovary (CHO) cells, zacopride activated the Kir2.1 homomeric channel but not the Kir2.2 or Kir2.3 channels [3].
体内活性	In all the three treatment modes, zacopride (15 μg/kg) inhibited MI-induced ventricular tachyarrhythmias, as shown by significant decreases in the premature ventricular contraction (PVC) and the duration and incidence of VT or VF [3]. Zacopride enhanced exploratory behaviour and social interaction in the mouse and rat models and antagonized the defensive response in the marmoset, zacopride being 100 times more potent than diazepam [4].
激酶实验	[3H] GR113808 binding studies were performed. Membranes were incubated at 37°C for 30 min in 0.5 ml of 50 mM Hepes pH 7.4 buffer, containing 0.1 nM [3H]GR113808, a specific ligand for 5-HT4 receptor, for the competition binding studies and varying concentrations of the radioligand for the saturation studies. Non-specific binding was defined with 30 μM 5-HT. For all binding studies, the incubation was terminated by rapid filtration and washing with ice-cold Hepes buffer through GF/B filters using a Brandel Cell Harvester. Radioactivity of the filter was counted [1].
细胞实验	In brief, a rat heart was quickly removed and mounted via the aorta on an 80-cm H2O high Langendorff retrograde perfusion apparatus. The heart was perfused first with oxygenated Ca2+-free Tyrode solution (at 37°C) for approximately 7–8 minutes, then with collagenase P (0.1 g/L) Tyrode solution for about 15 minutes. The composition of the Tyrode solution was (in millimoles per liter): NaCl 135, KCl 5.4, CaCl2 1.8, MgCl2 1.0, NaH2PO4 0.33, HEPES 10, glucose 10, pH adjusted to 7.3–7.4 with NaOH. When the tissue was well digested, the left ventricle was separated, minced and filtrated in KB solution with the following composition (in millimoles per liter): KOH 85, L-glutamic acid 50, KCl 30, MgCl2 1.0, KH2PO4 30, glucose 10, taurine 20, HEPES 10, ethylene glycol tetraacetic acid (EGTA), 0.5, pH adjusted to 7.4 with KOH. The isolated myocytes were stored at room temperature (23–25°C) at least 2 hours before use. The cell suspension was then transferred to a chamber mounted on an inverted microscope and superfused with the Tyrode solution. The whole-cell recording was performed with an amplifier Axopatch 200B. When filled with the pipette solution, the electrode resistance was maintained at 2–5 MΩ except for 1–1.5 MΩ for the Na+ current recording. The current signal was filtered at 2 kHz and sampled at 10– 20 kHz. Current was recorded in the voltage clamp mode, and membrane potentials were recorded in the current clamp mode at a frequency of 1.0 Hz. The baseline currents or APs were recorded first, then current values were recorded in the presence of zacopride at different concentrations (0.1, 1.0, 10 μmole/L). Ionic currents were corrected for cell capacitance and expressed in terms of current density (picoamperes/picofarads). All the experiments were conducted at room temperature (23–25°C), except at 36°C for AP recordings. The series resistance was 5.7 ± 2.2 MΩ, and the cell capacitance and pipette series resistance were mostly compensated (usually >70%) [2].
动物实验	Aconitine was administered into the exposed vena jugularis in the course of 10 seconds at a dosage of 30 μg/kg (0.046 μmole/kg). Then, 0.2 mL normal saline (NS) or zacopride at a dosage of 25 μg/kg (dissolved in NS, ~0.2 mL) or lidocaine at 7.5 mg/kg (dissolved in NS, ~0.2 mL) were administered immediately into the exposed left femoral vein (n = 8 in each group). In the pilot experiments, 25 μg/kg of zacopride and 7.5 mg/kg of lidocaine showed the optimal antiarrhythmic effects and fewer proarrhythmic side effects. The ECG signals were recorded continuously for a total of 1 hour after the administration of aconitine, and the arrhythmias were evaluated. Various arrhythmic activities, such as DADs, triggered activity (TA), premature ventricular contraction (PVC), ventricular tachycardia (VT), and ventricular fibrillation (VF) were monitored in the observed time window. Parameters of various arrhythmias, such as the episodes and the average duration of each type of arrhythmias, the incidence rate, and the total duration of the arrhythmias among groups, were calculated [2].

分子量	346.26
分子式	C15H20ClN3O2.HCl
CAS No.	101303-98-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (173.29 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.888 mL	14.44 mL	28.88 mL	72.2001 mL
	5 mM	0.5776 mL	2.888 mL	5.776 mL	14.44 mL
	10 mM	0.2888 mL	1.444 mL	2.888 mL	7.22 mL
	20 mM	0.1444 mL	0.722 mL	1.444 mL	3.61 mL
	50 mM	0.0578 mL	0.2888 mL	0.5776 mL	1.444 mL
	100 mM	0.0289 mL	0.1444 mL	0.2888 mL	0.722 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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配液浓度

参考文献

1. 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. 2. Liu QH, et al. A novel discovery of IK1 channel agonist: zacopride selectively enhances IK1 current and suppresses triggered arrhythmias in the rat. J Cardiovasc Pharmacol. 2012 Jan;59(1):37-48. 3. Zhai XW, et al. The IK1/Kir2.1 channel agonist zacopride prevents and cures acute ischemic arrhythmias in the rat. PLoS One. 2017 May 18;12(5):e20177600. 4. Costall B, et al. Zacopride: anxiolytic profile in rodent and primate models of anxiety. J Pharm Pharmacol. 1988 Apr;40(4):302-5.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Zacopride hydrochloride 101303-98-4 GPCR/G Protein Membrane transporter/Ion channel Neuroscience 5-HT Receptor Potassium Channel IK1 Serotonin Receptor Zacopride Hydrochloride 5-hydroxytryptamine Receptor Zacopride Inhibitor 5-HT4 ardiac protective 5-HT3 antiarrhythmic inhibit inhibitor

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Zacopride hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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