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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Zacopride hydrochloride targets serotonin 5-HT3 and 5-HT4 receptors. It is a highly potent 5-HT3 receptor antagonist with a Kd of 0.38 nM and a 5-HT4 receptor agonist with a Ki of 373 nM. It also acts as a selective IK1 channel agonist. By blocking 5-HT3 receptors and activating 5-HT4 receptors, the compound modulates serotonergic signaling pathways involved in nausea, emesis, anxiety, and gastrointestinal motility.
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| ln Vitro |
In vitro, Zacopride hydrochloride acts as a highly potent 5-HT3 receptor antagonist and a 5-HT4 receptor agonist. Its activity is typically assessed by measuring its ability to inhibit 5-HT-induced ion flux (for 5-HT3 antagonist activity) or stimulate cAMP accumulation (for 5-HT4 agonist activity) in cells expressing the respective receptors. The compound shows Ki values of 0.38 nM for 5-HT3 and 373 nM for 5-HT4 receptors. Standard in vitro assays include receptor binding studies using radiolabeled ligands and functional assays measuring ion flux or cAMP accumulation.
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| ln Vivo |
In vivo, Zacopride hydrochloride is a potent anxiolytic in animal models and has strong antiemetic effects. It increases aldosterone levels via activation of 5-HT4 receptors in the adrenal glands. The compound has been studied for its potential in treating anxiety disorders, emesis, and psychiatric conditions. It has potential research value for schizophrenia. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Zacopride hydrochloride can be evaluated using membrane preparations from cells expressing human 5-HT3 or 5-HT4 receptors. Radioligand binding displacement experiments are performed using suitable radiolabeled ligands such as [3H]-GR65630 for 5-HT3 or [3H]-GR113808 for 5-HT4. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ligand. Ki or Kd values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human 5-HT3 or 5-HT4 receptors are cultured in appropriate media. For 5-HT3 antagonist assays, calcium influx is measured using fluorescent calcium indicators. Cells are loaded with the dye and pre-incubated with various concentrations of Zacopride hydrochloride. Receptor activation is stimulated by the addition of a 5-HT3 receptor agonist. For 5-HT4 agonist assays, cAMP accumulation is measured. Cells are treated with various concentrations of the compound, and cAMP levels are measured using ELISA or HTRF-based detection. EC50 or IC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, Zacopride hydrochloride can be administered to rodents via intraperitoneal injection. In models of anxiety (e.g., elevated plus maze, social interaction test), behavioral responses are assessed following compound administration. In models of emesis, the compound's antiemetic effects are evaluated. In models of psychiatric disorders, behavioral tests are conducted. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Zacopride hydrochloride has a molecular weight of 346.25 and a molecular formula of C15H21Cl2N3O2. It is supplied with a purity of ≥98%. The compound is soluble in appropriate solvents for research use. It should be stored at -20°C for long-term stability. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of Zacopride hydrochloride has not been extensively reported. As a 5-HT3 receptor antagonist and 5-HT4 receptor agonist, potential adverse effects may include modulation of serotonergic signaling, which could affect gastrointestinal motility, mood, and aldosterone levels. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies.
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| References |
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| Additional Infomation |
See also: Zacopride Hydrochloride (note moved to).
Zacopride hydrochloride (CAS 101303-98-4) is a highly potent 5-HT3 receptor antagonist (Kd = 0.38 nM) and a 5-HT4 receptor agonist (Ki = 373 nM). It is a sub-nanomolar antagonist of the serotonin 5-HT3 receptor that also displays agonist-like activity against 5-HT4 receptors. It is a potent anxiolytic in animal models, has strong antiemetic effects, and increases aldosterone levels via activation of 5-HT4 receptors. It is available for research purposes only. |
| Molecular Formula |
C15H21CL2N3O2
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|---|---|
| Molecular Weight |
346.25
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| Exact Mass |
345.101
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| CAS # |
101303-98-4
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| PubChem CID |
9928181
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| Appearance |
White to off-white solid powder
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| Melting Point |
158-160 °C
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| LogP |
3.65
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
387
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N.Cl
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| InChi Key |
ITXVOUSORXSTQH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H20ClN3O2.ClH/c1-21-14-7-12(17)11(16)6-10(14)15(20)18-13-8-19-4-2-9(13)3-5-19;/h6-7,9,13H,2-5,8,17H2,1H3,(H,18,20);1H
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| Chemical Name |
4-amino-N-(1-azabicyclo[2.2.2]octan-3-yl)-5-chloro-2-methoxybenzamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (288.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (7.22 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8881 mL | 14.4404 mL | 28.8809 mL | |
| 5 mM | 0.5776 mL | 2.8881 mL | 5.7762 mL | |
| 10 mM | 0.2888 mL | 1.4440 mL | 2.8881 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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