Home Tools

Zacopride hydrochloride

Catalog No. T5336 CAS 101303-98-4

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Zacopride hydrochloride Chemical Structure

Zacopride hydrochloride, CAS 101303-98-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 478.00
100 mg	In stock	$ 689.00
1 mL * 10 mM (in DMSO)	In stock	$ 123.00

Bulk Inquiry

Select Batch

Purity: 98.32%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	5-HT4:373 nM (Ki, cell free), 5-HT3:0.38 nM (Kd, cell free)
In vitro	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].
In vivo	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].
Kinase Assay	[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].
Cell Research	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].
Animal Research	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].

Molecular Weight	346.26
Formula	C15H20ClN3O2.HCl
CAS No.	101303-98-4

Storage

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

Solubility Information

DMSO: 60 mg/mL (173.29 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Membrane Protein-targeted Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Potassium Channel Blocker Library Serotonin Receptor-Targeted Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets

Margatoxin TFA KT-362 fumarate Iberiotoxin TFA PAP-1 H3B-120 Atpenin A5 Rosuvastatin Rabeprazole

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.