Size | Price | |
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100mg | ||
250mg | ||
500mg |
Targets |
H1 Receptor; antihistamine
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ln Vitro |
Meclizine (Meclozine; 50 µM; 24 hours) reportedly inhibits apoptosis in STHdh cells, as seen by the considerable increase in cell survival 24 hours after serum withdrawal (based on caspase 3 and 7 cleavage). With an EC50 of 17.3 µm, the rescue effect was dose-dependent. When comparing the highest efficacy to the vehicle, the survival rate increased by 218%. Meclizine prevents serum withdrawal-induced apoptosis in striatal cells expressing polyglutamine (polyQ)-amplified huntingtin in both mutant (STHdhQ111/111) and wild-type (STHdhQ7/7) striatal cells [2].
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ln Vivo |
Mice protected against renal ischemia by meclizine (Meclozine; 10-100 mg/kg; ip). It was demonstrated that pretreatment of mice's kidneys with 100 mg/kg Meclizine 17 or 24 hours prior to ischemia had a protective effect. Meclizine increases glycolysis and directly inhibits the Kennedy route of phosphatidylethanolamine production to lower mitochondrial oxygen consumption [4].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: Mouse striatal cells expressing wild-type (STHdhQ7/7) or mutant (STHdhQ111/111) huntingtin Tested Concentrations: 50 µM Incubation Duration: 24 hrs (hours) Experimental Results: Cells in STHdhQ111/111 Survival rates were Dramatically increased for cells 24 hrs (hours) after removal of serum. Western Blot Analysis[2] Cell Types: mutant (STHdhQ111/111) and wild type (STHdhQ7/7) Striatal cell Tested Concentrations: 50 µM Incubation Duration: 0, 4, 10, 24 hrs (hours) Experimental Results: Inhibition of apoptosis ( Based on caspase 3) and 7 cleavage. |
Animal Protocol |
Animal/Disease Models: 8-10 weeks old male C57BL/6 mice [4]
Doses: 10, 30, 60 or 100 mg/kg Route of Administration: intraperitonealadministration Experimental Results: Protect mice from renal ischemia-reperfusion injury . |
References |
[1]. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness.
[2]. Vishal M Gohil, et al. Meclizine is neuroprotective in models of Huntington's disease. Hum Mol Genet. 2011 Jan 15;20(2):294-300. [3]. Wendong Huang, et al. Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR [4]. Seiji Kishi, et al. Meclizine Preconditioning Protects the Kidney Against Ischemia-Reperfusion Injury. EBioMedicine. 2015 Jul 29;2(9):1090-101. |
Additional Infomation |
Meclizine is a histamine H1 antagonist with antiemetic and antivertigo properties. It is used in the symptomatic treatment of motion sickness and control of vertigo associated with vestibular system diseases. It also exhibits anticholinergic, central nervous system depressant, and local anesthetic effects. Commonly marketed under the brand name Antivert in the U.S., meclizine is available as oral tablets.
Meclizine is an Antiemetic. The physiologic effect of meclizine is by means of Emesis Suppression. Meclizine is a first generation antihistamine that is used largely to treat vertigo and motion sickness. Meclizine has not been linked to instances of clinically apparent acute liver injury. Meclizine is a synthetic piperazine with anti-emetic, sedative and histamine H1antagonistic properties. Meclizine blocks the H1 histamine receptor and prevents the symptoms that are caused by histamine activity on capillaries, bronchial and gastrointestinal smooth muscles, including vasodilation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscles. Meclizine hydrochloride may exert its antiemetic effects by its anticholinergic actions or due to a direct effect on the medullary chemoreceptive trigger zone. Meclizine is only found in individuals that have used or taken this drug. It is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. [PubChem]Along with its actions as an antagonist at H1-receptors, meclizine also possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine depresses labyrinth excitability and vestibular stimulation and may affect the medullary chemoreceptor trigger zone. A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. |
Molecular Formula |
C25H27N2CL
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Molecular Weight |
390.94828
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Exact Mass |
426.163
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Elemental Analysis |
C, 76.81; H, 6.96; Cl, 9.07; N, 7.17
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CAS # |
569-65-3
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Related CAS # |
Meclizine dihydrochloride;1104-22-9;Meclizine-d8 dihydrochloride;1432062-16-2;Meclizine dihydrochloride monohydrate;31884-77-2
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PubChem CID |
4034
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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Density |
1.159 g/cm3
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Boiling Point |
1.5 g/100 mL
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Melting Point |
153-157ºC
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Flash Point |
253.3ºC
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LogP |
6.5
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tPSA |
6.23
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SMILES |
CC1=CC(=CC=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl
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InChi Key |
OCJYIGYOJCODJL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C25H27ClN2/c1-20-6-5-7-21(18-20)19-27-14-16-28(17-15-27)25(22-8-3-2-4-9-22)23-10-12-24(26)13-11-23/h2-13,18,25H,14-17,19H2,1H3
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Chemical Name |
1-[(4-chlorophenyl)-phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine
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Synonyms |
meclizine; Meclozine; 569-65-3; HSDB3113; HSDB-3113; HSDB 3113; Parachloramine; Bonadettes; Histamethine; Histamethizine; Histametizine;
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5579 mL | 12.7894 mL | 25.5787 mL | |
5 mM | 0.5116 mL | 2.5579 mL | 5.1157 mL | |
10 mM | 0.2558 mL | 1.2789 mL | 2.5579 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.