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Submit ReviewZacopride hydrochloride
Description: Highly potent 5-HT3 antagonist; also 5-HT4 agonist
Chemical Name: (±)-4-Amino-N-1-azabicyclo[2.2.2]oct-3-yl-5-chloro-2-methoxybenzamide hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Highly potent 5-HT3 receptor antagonist (Ki = 0.38 nM) and 5-HT4 receptor agonist (Ki = 373 nM). Antiemetic and anxiolytic following systemic administration in vivo.
Compound Libraries
Zacopride hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 346.26 |
| Formula | C15H20ClN3O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 101303-98-4 |
| PubChem ID | 9928181 |
| InChI Key | ITXVOUSORXSTQH-UHFFFAOYSA-N |
| Smiles | Cl.COC1=C(C=C(Cl)C(N)=C1)C(=O)NC1CN2CCC1CC2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 34.63 | 100 | |
| DMSO | 34.62 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 346.26. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.89 mL | 14.44 mL | 28.88 mL |
| 5 mM | 0.58 mL | 2.89 mL | 5.78 mL |
| 10 mM | 0.29 mL | 1.44 mL | 2.89 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Cohen et al (1989) Comparison of the 5-HT3 receptor antagonist properties of ICS 205-930, GR38032F and zacopride. J.Pharmacol.Exp.Ther. 248 197 PMID: 2521513
Costall et al (1988) Zacopride: anxiolytic profile in rodent and primate models of anxiety. J.Pharm.Pharmacol. 40 302 PMID: 2900320
Kii and Ito (1997) Effects of 5-HT4-receptor agonists, cisapride, mosapride citrate, and zacopride, on cardiac action potentials in guinea pig isolated papillary muscles. J.Cardiovasc.Pharmacol. 29 670 PMID: 9213211
Nagakura et al (1999) Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacol.Res. 39 375 PMID: 10328995
If you know of a relevant reference for Zacopride hydrochloride, please let us know.
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Keywords: Zacopride hydrochloride, Zacopride hydrochloride supplier, 5-HT4, agonists, potent, 5-HT3, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, 1795, Tocris Bioscience
3 Citations for Zacopride hydrochloride
Citations are publications that use Tocris products. Selected citations for Zacopride hydrochloride include:
Ding et al (2015) The reinforcing effects of ethanol within the nucleus accumbens shell involve activation of local GABA and serotonin receptors. Toxins (Basel) 29 725 PMID: 25922425
Otvos et al (2015) Development of Plate Reader and On-Line Microfluidic Screening to Identify Ligands of the 5-Hydroxytryptamine Binding Protein in Venoms. Circulation 7 2336 PMID: 26114334
Wang et al (2016) 5-HTR3 and 5-HTR4 located on the mitochondrial membrane and functionally regulated mitochondrialfunctions Scientific Reports 6 37336 PMID: 27874067
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Literature in this Area
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Ion Channel Product Listing
A collection of around 500 products for ion channel research, the listing includes research tools for the study of:
- Ligand-gated ion channels
- Voltage-gated ion channels
- Other Ion Channels
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.