Toggle Nav
Close
  • Menu
  • Setting

Zacopride hydrochloride

Catalog No.
B6858
5-HT3 receptor antagonist and 5-HT4 receptor agonist
Grouped product items
SizePriceStock Qty
10mg
$143.00
In stock
50mg
$574.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist and 5-HT4 agonist (Ki values are 0.38 and 373 nM, respectively) [1]. 

5-HT3 and 5-HT4 receptors belong to 5-HT receptors which are a group of G protein-coupled receptor and ligand-gated ion channels located in the central and peripheral systems. 5-HT receptors play important roles in mediating both excitatory and inhibitory neurotransmission [1]. 

On perifused human adrenocortical slices, administration of 20-min pulses of zacopride (10-11 ~ 10-6 mol/L) induced aldosterone secretion in a dose-dependent manner. The minimal effective dose was 10-10 mol/L, and half-maximal stimulation was achieved at a dose of 7 × 10-8 mol/L [2]. 

In 28 healthy volunteers pretreated with dexamethasone, and then a single oral dose of placebo, 10 μg zacopride, or 400 μg zacopride, plasma aldosterone levels increased significantly within 90 min after the administration of 400 μg zacopride, remained elevated for 60 min, and gradually recovered to the baseline within 180 min. However, the administration of 10 μg zacopride or placebo did not modify the aldosterone concentration. No significant changes were observed in renin, adrenocorticotropic hormone, or cortisol levels [2]. 

References:

[1]. Nagakura Y, Akuzawa S, Miyata K, et al. Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacological Research, 1999, 39(5): 375-382.

[2]. Lefebvre H, Contesse V, Delarue C, et al. Effect of the serotonin-4 receptor agonist zacopride on aldosterone secretion from the human adrenal cortex: in vivo and in vitro studies. The Journal of Clinical Endocrinology and Metabolism, 1993, 77(6): 1662-1666.

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at RT
M.Wt346.26
Cas No.101303-98-4
FormulaC15H20ClN3O2·HCl
Solubilityinsoluble in EtOH; insoluble in H2O; ≥23.95 mg/mL in DMSO
Chemical Name4-amino-5-chloro-2-methoxy-N-((1R,3S,4R)-quinuclidin-3-yl)benzamide hydrochloride
SDFDownload SDF
Canonical SMILESClC(C=C(C(OC)=C1)C(N[C@H]2[C@H](CC3)CC[N@]3C2)=O)=C1N.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

Zacopride hydrochloride