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Zacopride hydrochloride

Product Name
Zacopride hydrochloride
CAS No.
101303-98-4
Chemical Name
Zacopride hydrochloride
Synonyms
Zacopride hydrochloride hydrate;4-Amino-N-1-azabicyclo[2.2.2]oct-3-yl-5-chloro-2-methoxybenzamide hydrochloride hydrate;IK1,5-HT Receptor,Serotonin Receptor,Zacopride hydrochloride,5-hydroxytryptamine Receptor,Zacopride,Inhibitor,5-HT4,ardiac protective,5-HT3,antiarrhythmic,inhibit
CBNumber
CB82401236
Molecular Formula
C15H21Cl2N3O2
Formula Weight
346.25
MOL File
101303-98-4.mol
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Zacopride hydrochloride Property

Melting point:
158-160 °C
storage temp. 
2-8°C
solubility 
H2O: ≥10mg/mL
form 
powder
color 
white to tan
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0081
Product name
Zacopride hydrochloride hydrate
Purity
≥98% (HPLC)
Packaging
10mg
Price
$163
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0081
Product name
Zacopride hydrochloride hydrate
Purity
≥98% (HPLC)
Packaging
50mg
Price
$658
Updated
2024/03/01
TRC
Product number
Z150708
Product name
ZacoprideHydrochloride
Packaging
50mg
Price
$610
Updated
2021/12/16
ApexBio Technology
Product number
B6858
Product name
Zacopridehydrochloride
Packaging
10mg
Price
$203
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0045883
Product name
ZACOPRIDE HYDROCHLORIDE
Purity
95.00%
Packaging
5MG
Price
$515
Updated
2021/12/16
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Zacopride hydrochloride Chemical Properties,Usage,Production

Uses

Zacopride Hydrochloride, is a highly potent SR-3 antagonist and SR-4 agonist. 5-HT3 receptor antagonist. Activates IK1 channel.

Biological Activity

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].[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.

Biochem/physiol Actions

Zacopride 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, and also has strong antiemetic effects, and also increases aldosterone levels via activation of 5-HT4 receptor in the adrenal glands.

storage

room temperature (desiccate)

Zacopride hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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101303-98-4, Zacopride hydrochlorideRelated Search:


  • 4-Amino-N-1-azabicyclo[2.2.2]oct-3-yl-5-chloro-2-methoxybenzamide hydrochloride hydrate
  • Zacopride hydrochloride hydrate
  • IK1,5-HT Receptor,Serotonin Receptor,Zacopride hydrochloride,5-hydroxytryptamine Receptor,Zacopride,Inhibitor,5-HT4,ardiac protective,5-HT3,antiarrhythmic,inhibit
  • 101303-98-4