| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
Alizapride HCl (Limican; Plitican; Vergentan; Superan; Alizaprida; Litican; MS-5080), the hydrochloride salt of alizapride which is a medication used for the theropy of nausea and vomiting, is a potent dopamine receptor antagonist with prokinetic and antiemetic effects.
| Targets |
Dopamine receptor
Dopamine D2 receptor [1] |
|---|---|
| ln Vitro |
In vitro activity: Alizapride has an N-allyl moiety, which means it may go through epoxidation, N-deallylation, or other reactions that lead to the formation of chemically reactive metabolites.[1]
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| ln Vivo |
Alizapride shows little toxicity (especially when administered parenterally) in mice and rats. In rodents and mice, alipride exhibits minimal toxicity (particularly when given topically). When administered orally or intravenously, Alizapride is primarily eliminated as an unchanged medication; however, approximately 25% of the drug goes through metabolic conversion prior to elimination. In rats, the aforementioned doses of apomorphine cause a decrease in gastrointestinal transit, which is counteracted by alisparid (5 mg/kg, s.c.).[2]
In a randomized double-blind crossover controlled trial involving cancer patients receiving chemotherapy, intravenous administration of Alizapride HCl (100 mg, administered 30 minutes before chemotherapy and repeated every 8 hours for 24 hours) exhibited significant antiemetic activity. It inhibited acute vomiting (within 24 hours post-chemotherapy) in 78% of patients, compared to 52% in the control group (metoclopramide) [1] - Alizapride HCl also reduced the frequency of vomiting episodes: the mean number of vomiting episodes per patient was 1.2 in the treatment group, significantly lower than the control group’s 3.5 [1] - The drug showed efficacy in controlling delayed vomiting (24–72 hours post-chemotherapy) in 65% of patients, which was comparable to the control group’s 60% [1] |
| Enzyme Assay |
A dopamine receptor antagonist with prokinetic and antiemetic properties, alizapride hydrochloride is also used to treat nausea and vomiting, including postoperative nausea and vomiting.
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| Animal Protocol |
Male Duncan–Hartley guinea pigs
Dosage: 2.5, 5, 10, 25 μg/kg Administration: Alizapride (2.5, 5, 10, 25 μg/kg; SC; 7 consecutive days) |
| Toxicity/Toxicokinetics |
Common adverse reactions reported in clinical trials included mild to moderate sedation (28% of patients), constipation (15%), and dry mouth (12%). These adverse reactions were all transient and resolved without discontinuation of the drug [1]. No significant abnormalities were observed in hematological parameters (red blood cells, white blood cells, platelets) or serum biochemical indicators (ALT, AST, creatinine, blood urea nitrogen) in patients receiving treatment [1].
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| References | |
| Additional Infomation |
Alizapride hydrochloride is the hydrochloride form of alisapride, a methoxy-2-benzamide derivative and dopamine 2 (D2) receptor antagonist with antiemetic effects. After administration, alisapride binds to and blocks the action of D2 receptors in the chemoreceptor trigger zone (CTZ) of the medulla oblongata, thereby preventing nausea and vomiting.
Alizapride hydrochloride is an antiemetic drug primarily used to prevent and treat nausea and vomiting caused by chemotherapy[1] - Its antiemetic mechanism is believed to be by competitively antagonizing dopamine D2 receptors in the brainstem chemoreceptor trigger zone (CTZ) to block the vomiting reflex[1] - Clinically, it is used to treat chemotherapy-induced vomiting, with a standard dose regimen of 100 mg intravenously before chemotherapy, followed by a repeat every 8 hours for 24 hours[1] - In trials, it showed superior efficacy and fewer adverse reactions (less extrapyramidal symptoms) compared to metoclopramide in controlling acute chemotherapy-induced vomiting.[1] |
| Molecular Formula |
C16H22CLN5O2
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|---|---|---|
| Molecular Weight |
351.83
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| Exact Mass |
351.146
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| Elemental Analysis |
C, 54.62; H, 6.30; Cl, 10.08; N, 19.91; O, 9.09
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| CAS # |
59338-87-3
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| Related CAS # |
Alizapride; 59338-93-1; Alizapride-13C,d3 hydrochloride
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| PubChem CID |
135497066
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| Appearance |
Solid powder
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| Density |
1.224 g/cm3
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| Boiling Point |
580.3ºC at 760 mmHg
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| Melting Point |
206-208°
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| Flash Point |
304.8ºC
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| LogP |
2.477
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
433
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BRECEDGYMYXGNF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H21N5O2.ClH/c1-3-6-21-7-4-5-11(21)10-17-16(22)12-8-13-14(19-20-18-13)9-15(12)23-2;/h3,8-9,11H,1,4-7,10H2,2H3,(H,17,22)(H,18,19,20);1H
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| Chemical Name |
6-methoxy-N-[(1-prop-2-enylpyrrolidin-2-yl)methyl]-3H-benzotriazole-5-carboxamide;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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 25.0 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: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (142.11 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8423 mL | 14.2114 mL | 28.4228 mL | |
| 5 mM | 0.5685 mL | 2.8423 mL | 5.6846 mL | |
| 10 mM | 0.2842 mL | 1.4211 mL | 2.8423 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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