Betahistine mesylate

Betahistine mesylate Basic information
Product Name:Betahistine mesylate
Synonyms:BETAHISTINE MESILATE;n-methyl-2-pyridineethanamindimethanesulfonate;2-[2-(METHYLAMINO)ETHYL]PYRIDINE METHANESULFONATE;BETAHISTINE MESYLATE;BETAHISTINE METHANESULFONATE;BETAHISTINE DIMESYLATE;BETAHISTINE DIMETHANESULFONATE;n-methyl-2-pyridineethylamine dimethanesulphonate
CAS:54856-23-4
MF:C8H12N2.2CH4O3S
MW:328.41
EINECS:259-377-7
Product Categories:Pharmaceutical raw material
Mol File:54856-23-4.mol
Betahistine mesylate Structure
Betahistine mesylate Chemical Properties
Melting point 112°C
storage temp. Keep in dark place,Inert atmosphere,Room temperature
solubility Very soluble in water, freely soluble in ethanol (96 per cent), very slightly soluble in 2-propanol.
form neat
color White to Off-White
Water Solubility almost transparency
Stability:Hygroscopic
CAS DataBase Reference54856-23-4(CAS DataBase Reference)
Safety Information
RTECS UT2970200
HS Code 2933.39.9200
ToxicityLD50 orl-rat: 3030 mg/kg NIIRDN 6,750,82
MSDS Information
Betahistine mesylate Usage And Synthesis
Chemical PropertiesWhite or almost white, crystalline powder, very hygroscopic.
UsesVasodilatator;H1 agonist
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).
DefinitionBetahistine mesylate is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
IndicationsBetahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
Safety ProfilePoison by subcutaneous route.Moderately toxic by ingestion and other routes. Whenheated to decomposition it emits toxic fumes of NOx andSOx.
in vitroIn Vitro: Betahistine mesylate (0-10 μM) inhibits [125I]iodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells with IC50 values of 1.9 μM and 3.3 μM, respectively. Lead to Ki values of 1.4 μM and 2.5 μM, respectively.
Betahistine mesylate (0-10 μM) has a regulating function on cAMP formation in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. At low concentrations, Betahistine mesylate behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC50 values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, Betahistine mesylate inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) and full agonist activity.
Mode of actionBetahistine is indicated for the treatment of Meniere's disease and other audiovestibular disorders like vertigo and tinnitus. Betahistine is an analogue of histamine and an H1-receptor agonist. Stimulating the H1- receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels, resulting in reduced endolymphatic pressure. Betahistine acts by reducing the asymmetrical functioning of sensory vestibular organs and increasing vestibulocochlear blood flow, decreasing symptoms of vertigo, tinnitus, balance disorders, and hearing loss associated with Meniere's disease. Betahistine also acts as a histamine H3- receptor antagonist which causes an increased output of histamine, increase in the direct H1-agonist activity, and inhibition of the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms.
Betahistine mesylate Preparation Products And Raw materials
Methylparaben Methyl Bensulfuron methyl 2-Chloro-5-chloromethylpyridine Dimethyldimethoxysilane Doxazosin mesylate Parathion-methyl Betahistine Azamethiphos Kresoxim-methyl 2,6-Lutidine Thiophanate-methyl Betahistine dihydrochloride Dimethyl methylphosphonate Methyl acrylate Methyl acetate Methyl bromide 4-Dimethylaminopyridine

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