Name | meclizine dihydrochloride |
Synonyms | Meclozine Hcl Meclizine hcl Meclizine 2HCl Meclizine hydrochloride meclozine dihydrochloride Meclizine dihydrochloride meclizine dihydrochloride 1-p-chlorbenzhydryl-m-methylbenzylpiperazinedihydrochloride 1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine 1-(p-Chloro-α-phenylbenzyl)-4-(m-methylbenzyl)-piperazine dihydrochloride 1-((4-Chlorophenyl)(phenyl)Methyl)-4-(3-Methylbenzyl)piperazine dihydrochloride 1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine dihydrochloride Piperazine, 1-[(4-chlorophenyl)phenylmethyl]-4-[(3-methylphenyl)methyl]-, dihydrochloride |
CAS | 1104-22-9 |
EINECS | 214-164-8 |
InChI | InChI=1/C25H27ClN2.ClH/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;1H |
Molecular Formula | C25H29Cl3N2 |
Molar Mass | 463.87 |
Melting Point | 210.0 to 214.0 °C |
Boling Point | 495.3°C at 760 mmHg |
Flash Point | 253.3°C |
Solubility | DMSO: soluble5mg/mL, clear (warmed) |
Vapor Presure | 6E-10mmHg at 25°C |
Appearance | White, slightly yellowish, crystalline powder |
Color | white to beige |
Storage Condition | 2-8°C |
In vitro study | Meclizine is a histamine H1 receptor antagonist used in the treatment of Nausea and motion sickness with anticholinergic, central nervous system depressant and local anesthetic effects. Meclizine is a mouse CAR agonist ligand (constitutive androstane receptor), an inverse agonist of the human CAR. In vitro experiments, Meclizine dose-dependently increased mCAR transactivation, activating the binding of hormone receptor coactivator 1 to the receptor. In contrast, in mouse-derived liver cells that express only hCAR but do not express mCAR, meclizine inhibits transcriptional activation of hCAR and Lumina-induced CAR downstream genes, including the expression of cytochrome p450 monooxygenase (CYP)2B10,CYP3A11, and CYP1A2. |
In vivo study | Treatment of mice with Meclizine increased CAR target gene expression in a CAR-dependent manner. In the mouse polyQ toxicity cell model, Meclizine reduces oxidative metabolism and inhibits apoptotic cell death. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R63 - Possible risk of harm to the unborn child |
Safety Description | S22 - Do not breathe dust. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | TL2005000 |
Toxicity | LD50 oral in mouse: 1600mg/kg |
Reference Show more | 1. Li, Meng, et al. "Chiral separation of five antihistamine drug enantiomers and enantioselective pharmacokinetic study of carbinoxamine in rat plasma by HPLC-MS/MS." New Journal of Chemistry 44.15 (2020): 5819-5827.https://doi.org/10.1039/D0NJ00095G 2. [IF=3.591] Meng Li et al."Chiral separation of five antihistamine drug enantiomers and enantioselective pharmacokinetic study of carbinoxamine in rat plasma by HPLC-MS/MS."New J Chem. 2020 Apr;44(15):5819-5827 |
This product is l-[(4-chlorophenyl) benzyl]-4-[(3-tolyl) methyl] piperazine dihydrochloride. The content of C25H27C1N2 • 2HC1 shall not be less than 97.0% calculated as anhydrous.
take this product, precision weighing, plus O. 1 mol/L hydrochloric acid solution is dissolved and quantitatively diluted to prepare a solution containing about 15ug per 1 ml, and the absorbance is measured at the wavelength of 232mn by ultraviolet-visible spectrophotometry (General rule 0401), the absorption coefficient is 345 to 380.
take 0.20g of this product, add 0901 ethanol to dissolve, the solution should be clear and colorless; If the color is colored, check according to law (General rule first law), and compare with the yellow No. 2 Standard Colorimetric solution, not deeper.
take this product, add methylene chloride-methanol (1:1) dissolved and diluted to make a solution containing about 50mg per 1 ml, as a solution for the test sample; Take an appropriate amount of precision, as a control solution, a solution containing 0502 mg per 1 ml was prepared by quantitative dilution with dichloromethane-methanol (1:1); As tested by thin layer chromatography (general), draw 10 u1 of each of the above two solutions, respectively, on the same silica gel G thin layer plate, with dichloromethane-toluene-methanol-concentrated ammonia solution (60:30:5:0.5) as the developing solvent, it was developed, dried, and sprayed with dilute bismuth potassium iodide solution. Test solution such as impurity spots, compared with the control solution of the main spot, not deeper.
take this product, according to the determination of moisture (General 0832 first method 1), the water content shall not exceed 5.0%.
not more than 0.1% (General rule 0841).
take about 0.2g of this product, precision weighing, add chloroform 50ml to dissolve, add glacial acetic acid 50ml, acetic anhydride 5ml and Mercury acetate test solution 10ml, according to the potential titration method (General rule 0701), with perchloric acid titration solution (O. 1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 23.19mg of C25H27C1N2 · 2HC1.
antihistamines.
light shielding, sealed storage.
This product contains meclizine hydrochloride (C25H27C1N2 • 2HC1) should be 90.0% ~ 110.0% of the label.
This product is from yellowish to yellowish.
should be in accordance with the relevant provisions under The tablet item (General rule 0101).
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (about 0.2g equivalent to Meclozine hydrochloride), place it in a separatory funnel, add 50ml of water, shake, extract with chloroform 50ml, 20ml and 20ml respectively for 3 times, combine chloroform solution, put on a water bath to evaporate 10 ~ 15ml, let cool, add glacial acetic acid 15ml, acetic anhydride 5ml, mercury acetate test solution 5ml and dipteridine red indicator solution 2 drops, with perchloric acid titration solution (O. 1 mol/L) titration until the red color disappeared, and the titration results were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 23.19mg of C25H27C1N2 · 2HC1.
with Meclozine hydrochloride.
25mg
light shielding, sealed storage.