Zacopride hydrochloride

Name: Zacopride hydrochloride
Brand: MedChemExpress
SKU: HY-103137
Rating: 4.5 (1 reviews)

Cat. No.: HY-103137 Purity: 99.69%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Zacopride hydrochloride is an orally active 5-HT₃ receptor (K_i of 0.38 nM) antagonist and 5-HT₄ receptor (K_i of 373 nM) agonist. Zacopride hydrochloride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride hydrochloride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety.

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Zacopride hydrochloride 화학구조

CAS No. : 101303-98-4

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of Zacopride hydrochloride:

Zacopride 견적 받기
Zacopride hydrochloride (Standard) 견적 받기

1 Publications Citing Use of MCE Zacopride hydrochloride

•Front Immunol. 2026 Jan 12:16:1683500. [Abstract]

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5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
순도&문서
References
고객리뷰

제품 설명

In Vitro

Zacopride (3-30 μM) hydrochloride reduces the 5-HT-induced maximum contraction response of guinea pig colon in a concentration-dependent manner^[3].
Zacopride hydrochloride produces 5-HT₄ receptor-mediated relaxation of the rat esophagus with an EC₅₀ value of 0.5 μM^[3].
Zacopride hydrochloride (10 μM) shortens duration of action potentials in guinea pig isolated papillary muscles^[11].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Zacopride (0.1 mg/kg; p.o.; single dose) hydrochloride can induce vomiting in ferrets^[4].
Zacopride (0.1 mg/kg; intraperitoneal injection; single dose) hydrochloride can completely block the vomiting induced by oral administration of 0.1 mg/kg Zacopride in ferrets^[4].
Zacopride hydrochloride (0.1 mg/kg; intraperitoneal injection; single dose) hydrochloride can significantly attenuate the increase in extracellular dopamine levels in the nucleus accumbens induced by cocaine in rats^[5].
Zacopride (Zacopride chlorhydrate, 1.0 mg/kg; intraperitoneal injection; single dose) hydrochloride combined with Tacrine can improve the accuracy of rats at the shortest delay (0-4 s) in a spatial working memory task^[6].
Zacopride hydrochloride (0.01-31.6 mg/kg; p.o.; multiple doses until vomiting occurs) induces vomiting in 100% of ferrets at a cumulative dose of 0.11 mg/kg^[7].
Zacopride hydrochloride (0.5 mg/kg; intravenous injection; single dose) combined with Etorphine can alleviate the decrease in respiratory rate caused by Etorphine in goats, increase hemoglobin oxygen saturation and arterial oxygen tension, while reducing carbon dioxide tension and improving ventilation^[8].
Zacopride (0.1-1.0 mg/kg; intraperitoneal injection; single dose) hydrochloride exhibits anxiolytic effects in mice (social interaction and elevated plus maze test)^[9].
Zacopride (0.0001-10 mg/kg; intraperitoneal injection; single dose) hydrochloride can enhance the exploratory behavior (black-white test box test) and social interaction (social interaction test with rats) of mice^[10].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Kuo:Wistar rats (weight: at the beginning of training, 3-month-old rats were used, weight information not specified further), spatial working memory task model^[6].
Dosage:	0.0025-1.0 mg/kg (intraperitoneal, zacopride); 1.0 mg/kg (intraperitoneal, zacopride in combination with tacrine)
Administration:	Intraperitoneal injection (single dose)
Result:	Had no significant effect on the percent correct responses in the spatial working memory task at 0.0025-1.0 mg/kg. Increased the percent correct responses at the shortest delays (0-4 s) but not at the longest delays (8-30 s) when combined with Tacrine (1.0 mg/kg).

분자량

346.25

화학식

C₁₅H₂₁Cl₂N₃O₂

CAS No.

101303-98-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CN2CCC1CC2)C3=CC(Cl)=C(N)C=C3OC.[H]Cl

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도

In Vitro:

DMSO : 100 mg/mL (288.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (7.22 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.69%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (250 KB) LCMS (256 KB)

Handling Instructions (2659 KB)

References

[1]. Neumann J, et al. Zacopride stimulates 5-HT4 serotonin receptors in the human atrium. Naunyn Schmiedebergs Arch Pharmacol. 2024 Sep;397(9):6821-6835. [Content Brief]

[2]. Pinkus L M, et al. Utilization of Zacopride and its R-and S-Enantiomers in Studies of 5-HT 3 Receptor “Subtypes”. Serotonin: Molecular Biology, Receptors and Functional Effects, 1991: 439-448.

[3]. Nagakura Y, et al. Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor. Pharmacol Res. 1999 May;39(5):375-82. [Content Brief]

[4]. Sancilio LF, et al. Emetic activity of zacopride in ferrets and its antagonism by pharmacological agents. Eur J Pharmacol. 1990 Jun 8;181(3):303-6. [Content Brief]

[5]. McNeish CS, et al. The 5-HT3 antagonist zacopride attenuates cocaine-induced increases in extracellular dopamine in rat nucleus accumbens. Pharmacol Biochem Behav. 1993 Aug;45(4):759-63. [Content Brief]

[6]. Jäkälä P, et al. The effects of tacrine and zacopride on the performance of adult rats in the working memory task. Gen Pharmacol. 1993 May;24(3):675-9. [Content Brief]

[7]. Sancilio LF, et al. Studies on the emetic and antiemetic properties of zacopride and its enantiomers. Eur J Pharmacol. 1991 Jan 17;192(3):365-9. [Content Brief]

[8]. Meyer LC, et al. Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats. Am J Physiol Regul Integr Comp Physiol. 2006 Feb;290(2):R405-13. [Content Brief]

[9]. Dunn R W, et al. Preclinical anxiolytic versus antipsychotic profiles of the 5‐HT3 antagonists ondansetron, zacopride, 3α‐tropanyl‐1H‐indole‐3‐carboxylic acid ester, and 1αH, 3α, 5αH‐tropan‐3‐yl‐3, 5‐dichlorobenzoate. Drug development research, 1991, 23(4): 289-300.

[10]. Costall B, et al. Zacopride: anxiolytic profile in rodent and primate models of anxiety. J Pharm Pharmacol. 1988 Apr;40(4):302-5. [Content Brief]

[11]. Kii Y, et al. Effects of 5-HT4-receptor agonists, cisapride, mosapride citrate, and zacopride, on cardiac action potentials in guinea pig isolated papillary muscles. J Cardiovasc Pharmacol. 1997 May;29(5):670-5. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8881 mL	14.4404 mL	28.8809 mL	72.2022 mL
	5 mM	0.5776 mL	2.8881 mL	5.7762 mL	14.4404 mL
	10 mM	0.2888 mL	1.4440 mL	2.8881 mL	7.2202 mL
	15 mM	0.1925 mL	0.9627 mL	1.9254 mL	4.8135 mL
	20 mM	0.1444 mL	0.7220 mL	1.4440 mL	3.6101 mL
	25 mM	0.1155 mL	0.5776 mL	1.1552 mL	2.8881 mL
	30 mM	0.0963 mL	0.4813 mL	0.9627 mL	2.4067 mL
	40 mM	0.0722 mL	0.3610 mL	0.7220 mL	1.8051 mL
	50 mM	0.0578 mL	0.2888 mL	0.5776 mL	1.4440 mL
	60 mM	0.0481 mL	0.2407 mL	0.4813 mL	1.2034 mL
	80 mM	0.0361 mL	0.1805 mL	0.3610 mL	0.9025 mL
	100 mM	0.0289 mL	0.1444 mL	0.2888 mL	0.7220 mL