| Size | Price | Stock | Qty |
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| 250mg |
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| 5g |
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Purity: ≥98%
Metoclopramide HCl is a potent and selective dopamine D2 receptor antagonist. It is a medication used mostly for stomach and esophageal problems such as nausea and vomiting. It can help with emptying of the stomach in people with delayed stomach emptying due to either diabetes or following surgery, and help with gastroesophageal reflux disease. In addition, it can also used to treat migraine headaches.
| ln Vitro |
Aldosterone release in isolated rat glomerular zona perfused cells is stimulated by metoclopramide (0.01-10 μM) [3]. Acetylcholine (ACh) is released from intrinsic cholinergic motor neurons through four mechanisms that metoclopramide causes: inhibition of presynaptic D2 receptors, stimulation of presynaptic excitatory 5-HT4 receptors, inhibition of D2 postsynaptic receptors, and antagonism of presynaptic inhibition of muscarinic receptors, which leads to an additional increase in acetylcholine release [2].
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| ln Vivo |
Throughout the whole estrous cycle, metoclopramide (6.7 µg/g; daily subcutaneous injection for 50 days) dramatically raises pituitary prolactin cell volume and quantity [4]. Mice treated intraperitoneally with metoclopramide (5–40 mg/kg) exhibit catalepsy and are less likely to climb their cages in response to apomorphine [5]. Mice that receive an intraperitoneal dose of metoclopramide (1.25–2.5 mg/kg) may exhibit a stereotypical behavior of climbing cages [5].
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| Animal Protocol |
Animal/Disease Models: Adult female mice of Swiss EPM-1 strain [4]
Doses: 6.7 µg/g Route of Administration: daily subcutaneous injection for 50 days Experimental Results: Increased the amount of prolactin and also stimulated its metabolic activity. |
| 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 (
[2]. Rao AS, et, al. Review article: metoclopramide and tardive dyskinesia. Aliment Pharmacol Ther. 2010 Jan;31(1):11-9. [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. [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. [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. |
| Molecular Formula |
C14H22CLN3O2
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|---|---|
| Molecular Weight |
299.7964
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| CAS # |
364-62-5
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| Related CAS # |
Metoclopramide hydrochloride hydrate;54143-57-6;Metoclopramide hydrochloride;7232-21-5
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| SMILES |
ClC1=C(C([H])=C(C(=C1[H])C(N([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)OC([H])([H])[H])N([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~110 mg/mL (~366.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (9.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (9.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3356 mL | 16.6778 mL | 33.3556 mL | |
| 5 mM | 0.6671 mL | 3.3356 mL | 6.6711 mL | |
| 10 mM | 0.3336 mL | 1.6678 mL | 3.3356 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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