CAS 54856-23-4|Betahistine Mesylate

Introduction：Basic information about CAS 54856-23-4|Betahistine Mesylate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Betahistine Mesylate BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Articles25
8. Synonyms

Common Name	Betahistine Mesylate
CAS Number	54856-23-4	Molecular Weight	328.406
Density	/	Boiling Point	210.9ºC at 760 mmHg
Molecular Formula	C₁₀H₂₀N₂O₆S₂	Melting Point	112°C
MSDS	/	Flash Point	96.7ºC

Names

Name	Betahistine Mesylate
Synonym	More Synonyms

Betahistine Mesylate BiologicalActivity

Description	Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine mesylate is used for the study of rheumatoid arthritis (RA)[3].
Related Catalog	Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Histamine Receptor
In 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[2]. 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[2].
In Vivo	Betahistine mesylate (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50 of 2 mg/kg in male Swissmice[2]. Betahistine mesylate (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice[3]. Animal Model: Collagen-induced arthritis (CIA) DBA/1 male mouse model[3] Dosage: 1 mg/kg; 5mg/kg Administration: Oral adminstration; day 21 to day 42 after a 21-day CIA induction Result: Ameliorated mouse CIA by decreasing joint destruction.
References	[1]. Poyurovsky M, et al. The effect of Betahistine mesylate, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. [2]. Gbahou F, et al. Effects of Betahistine mesylate at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54. [3]. Tang KT, et al. Betahistine mesylate attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245

Chemical & Physical Properties

Boiling Point	210.9ºC at 760 mmHg
Melting Point	112°C
Molecular Formula	C₁₀H₂₀N₂O₆S₂
Molecular Weight	328.406
Flash Point	96.7ºC
Exact Mass	328.076263
PSA	150.42000
LogP	2.40400
InChIKey	ZBJJDYGJCNTNTH-UHFFFAOYSA-N
SMILES	CNCCc1ccccn1.CS(=O)(=O)O.CS(=O)(=O)O

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT2970200

CHEMICAL NAME :: 2-Pyridineethanamine, N-methyl-, dimethanesulfonate

CAS REGISTRY NUMBER :: 54856-23-4

LAST UPDATED :: 198212

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C8-H12-N2.2C-H4-O3-S

MOLECULAR WEIGHT :: 328.44

WISWESSER LINE NOTATION :: T6NJ A2M1 &QSW1 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3030 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 940 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 604 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1630 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 505 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 120 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 22900 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,750,1982

Safety Information

RTECS	UT2970200
HS Code	2933399090

Customs

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles25

Comparison of the therapeutic efficacy of a fixed low-dose combination of cinnarizine and dimenhydrinate with betahistine in vestibular neuritis: a randomized, double-blind, non-inferiority study.

Clin. Drug Investig. 32(6) , 387-99, (2012)

Vestibular neuritis (VN) is a strongly disabling disease of the peripheral vestibular system. Rapid and effective relief of symptoms is important to allow patients to promptly return to normal physica...

Betahistine or Cinnarizine for treatment of Meniere's disease.

Med. Arh. 66(6) , 396-8, (2012)

Meniere's disease is a condition with sudden attacks of vertigo with nausea and vomiting accompanied by loss of hearing and buzzing sensation in the ears, most commonly unilateral. The exact cause of ...

Vestibular rehabilitation with virtual reality in Ménière's disease.

Braz. J. Otorhinolaryngol. 79(3) , 366-74, (2013)

Virtual reality technology can provide a wide range of sensory stimuli to generate conflicts of varying degrees of complexity in a safe environment.To verify the effect of a virtual realitybased balan...

Synonyms

2-Pyridineethanamine, N-methyl-, methanesulfonate (1:2)

N-Methyl-2-pyridineethanamine Dimethanesulfonate

MFCD00211321

N-Methyl-2-(2-pyridinyl)ethanamine methanesulfonate (1:2)

EINECS 259-377-7

N-Methyl-2-(pyridin-2-yl)ethanamine methanesulfonate (1:2)

methanesulfonic acid,N-methyl-2-pyridin-2-ylethanamine

Recommended......