Metoclopramide hydrochloride hydrate
Based on 2 publication(s) in Google Scholar
Metoclopramide hydrochloride hydrate is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 54143-57-6
- Formula: C14H25Cl2N3O3
- Molecular Weight:354.27
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Metoclopramide hydrochloride hydrate
MoreAll 5-HT Receptor Isoforms
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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5-HT3 Receptor 308 nM (IC50) |
D2 Receptor 483 nM (IC50) |
Metoclopramide (0.01-10 μM) hydrochloride hydrate stimulates aldosterone release in isolated perfused rat zona glomerulosa cells[3].
Metoclopramide hydrochloride hydrate results in prokinesis by four mechanisms: inhibition of presynaptic D2 receptors and stimulation of presynaptic excitatory 5-HT4 receptors, thereby allowing acetylcholine (ACh) release from intrinsic cholinergic motor neurons; inhibition of D2 postsynaptic receptors; and antagonism of the presynaptic inhibition of muscarinic receptors, leading to further augmentation of ACh release[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Metoclopramide (5-40 mg/kg; i.p.) hydrochloride hydrate induces catalepsy and antagonizes Apomorphine induced cage climbing behaviour in mice[5].
Metoclopramide (1.25-2.5 mg/kg; i.p.) hydrochloride hydrate induces stereotyped cage climbing behaviour in mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult, virgin female mice of the Swiss EPM-1 strain[4]
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Dosage:6.7 µg/g
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Administration:S.c. daily for 50 days
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Result:Increased the number but also stimulated the metabolic activity of lactotrophs.
Chemical Information
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CAS No. 54143-57-6
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Appearance Solid
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Molecular Weight 354.27
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Formula C14H25Cl2N3O3
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Color White to off-white
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SMILES
O=C(NCCN(CC)CC)C1=CC(Cl)=C(N)C=C1OC.[H]Cl.[H]O[H]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Omega
Computational Approaches to Identify Molecules Binding to Mycobacterium tuberculosis KasA. [Abstract]2020 Nov 15;5(46):29935-29942. PMID: 33251429 -
Eur J Drug Metab Pharmacokinet
Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans. [Abstract]2022 Sep;47(5):639-652. PMID: 35733077
Solvent & Solubility
DMSO : 50 mg/mL (141.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.06 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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 and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hirokawa Y, et, al. Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist. Chem Pharm Bull (Tokyo). 2002 Jul;50(7):941-59. [Content Brief]
[2]. Rao AS, et, al. Review article: metoclopramide and tardive dyskinesia. Aliment Pharmacol Ther. 2010 Jan;31(1):11-9. [Content Brief]
[3]. Edwards CR, et, al. In vivo and in vitro studies on the effect of metoclopramide on aldosterone secretion. Clin Endocrinol (Oxf). 1980 Jul;13(1):45-50. [Content Brief]
[4]. Bhosale KB, et, al. Dose-dependent response of central dopaminergic systems to metoclopramide in mice. Indian J Exp Biol. 1997 Jun;35(6):618-22. [Content Brief]
[5]. Gomes RCT, et, al. Effects of metoclopramide on the mouse anterior pituitary during the estrous cycle. Clinics (Sao Paulo). 2011;66(6):1101-4. [Content Brief]
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.8227 mL | 14.1135 mL | 28.2271 mL | 70.5676 mL |
| 5 mM | 0.5645 mL | 2.8227 mL | 5.6454 mL | 14.1135 mL | |
| 10 mM | 0.2823 mL | 1.4114 mL | 2.8227 mL | 7.0568 mL | |
| 15 mM | 0.1882 mL | 0.9409 mL | 1.8818 mL | 4.7045 mL | |
| 20 mM | 0.1411 mL | 0.7057 mL | 1.4114 mL | 3.5284 mL | |
| 25 mM | 0.1129 mL | 0.5645 mL | 1.1291 mL | 2.8227 mL | |
| 30 mM | 0.0941 mL | 0.4705 mL | 0.9409 mL | 2.3523 mL | |
| 40 mM | 0.0706 mL | 0.3528 mL | 0.7057 mL | 1.7642 mL | |
| 50 mM | 0.0565 mL | 0.2823 mL | 0.5645 mL | 1.4114 mL | |
| 60 mM | 0.0470 mL | 0.2352 mL | 0.4705 mL | 1.1761 mL | |
| 80 mM | 0.0353 mL | 0.1764 mL | 0.3528 mL | 0.8821 mL | |
| 100 mM | 0.0282 mL | 0.1411 mL | 0.2823 mL | 0.7057 mL |
Metoclopramide hydrochloride hydrate Related Classifications
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