Zacopride hydrochloride

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Cat.No. 1795 - Zacopride hydrochloride | C15H20ClN3O2.HCl | CAS No. 101303-98-4
Description: Highly potent 5-HT3 receptor 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)
Citations (3)

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 34.62 100
ethanol 25.96 75
water 34.63 100
phosphate buffered saline 34.63 100

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 solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet


References are publications that support the products' biological activity.

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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3 Citations for Zacopride hydrochloride

Citations are publications that use Tocris products. Selected citations for Zacopride hydrochloride include:

Wang et al (2016) 5-HTR3 and 5-HTR4 located on the mitochondrial membrane and functionally regulated mitochondrialfunctions Scientific Reports 6 37336 PMID: 27874067

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

Do you know of a great paper that uses Zacopride hydrochloride from Tocris? If so please let us know.

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Literature in this Area

5-HT Receptors

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.