Betahistine Dihydrochloride

Modify Date: 2024-01-02 13:22:47

Betahistine Dihydrochloride Structure
Betahistine Dihydrochloride structure
Common Name Betahistine Dihydrochloride
CAS Number 5579-84-0 Molecular Weight 209.116
Density 0.967 g/cm3 Boiling Point 210.9ºC at 760 mmHg
Molecular Formula C8H14Cl2N2 Melting Point 150-154 °C
MSDS USA Flash Point 96.7ºC

 Use of Betahistine Dihydrochloride


Betahistine Dihydrochloride is a histamine H3 receptors inhibitor used as an antivertigo drug.Target: Histamine ReceptorBetahistine, a structural analogue of histamine with weak histamine H(1) receptor agonist and more potent H(3) receptor antagonist properties. Betahistine acts centrally by enhancing histamine synthesis within tuberomammillary nuclei of the posterior hypothalamus and histamine release within vestibular nuclei through antagonism of H(3) autoreceptors [1].Therapeutic effects of betahistine in vestibular disorders result from its antagonist properties at histamine H(3) receptors (H(3)Rs). On inhibition of cAMP formation and [(3)H]arachidonic acid release, betahistine behaved as a nanomolar inverse agonist and a micromolar agonist. After acute oral administration, Betahistine increased t-MeHA levels with an ED(50) of 2 mg/kg, a rightward shift probably caused by almost complete first-pass metabolism. Therapeutic effects of betahistine result from an enhancement of histamine neuron activity induced by inverse agonism at H(3) autoreceptors [2].

 Names

Name Betahistine dihydrochloride
Synonym More Synonyms

 Betahistine Dihydrochloride Biological Activity

Description Betahistine Dihydrochloride is a histamine H3 receptors inhibitor used as an antivertigo drug.Target: Histamine ReceptorBetahistine, a structural analogue of histamine with weak histamine H(1) receptor agonist and more potent H(3) receptor antagonist properties. Betahistine acts centrally by enhancing histamine synthesis within tuberomammillary nuclei of the posterior hypothalamus and histamine release within vestibular nuclei through antagonism of H(3) autoreceptors [1].Therapeutic effects of betahistine in vestibular disorders result from its antagonist properties at histamine H(3) receptors (H(3)Rs). On inhibition of cAMP formation and [(3)H]arachidonic acid release, betahistine behaved as a nanomolar inverse agonist and a micromolar agonist. After acute oral administration, Betahistine increased t-MeHA levels with an ED(50) of 2 mg/kg, a rightward shift probably caused by almost complete first-pass metabolism. Therapeutic effects of betahistine result from an enhancement of histamine neuron activity induced by inverse agonism at H(3) autoreceptors [2].
Related Catalog
References

[1]. Lacour, M. and O. Sterkers, Histamine and betahistine in the treatment of vertigo: elucidation of mechanisms of action. CNS Drugs, 2001. 15(11): p. 853-70.

[2]. Gbahou, F., et al., Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo. J Pharmacol Exp Ther, 2010. 334(3): p. 945-54.

 Chemical & Physical Properties

Density 0.967 g/cm3
Boiling Point 210.9ºC at 760 mmHg
Melting Point 150-154 °C
Molecular Formula C8H14Cl2N2
Molecular Weight 209.116
Flash Point 96.7ºC
Exact Mass 208.053406
PSA 24.92000
LogP 2.83840

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes Xi
Safety Phrases S24/25
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS UT2969000
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%

 Articles27

More Articles
Differential thermodynamic driving force of first- and second-generation antihistamines to determine their binding affinity for human H1 receptors.

Biochem. Pharmacol. 91(2) , 231-41, (2014)

Differential binding sites for first- and second-generation antihistamines were indicated on the basis of the crystal structure of human histamine H1 receptors. In this study, we evaluated differences...

Development of novel sustained release matrix pellets of betahistine dihydrochloride: effect of lipophilic surfactants and co-surfactants.

Pharm. Dev. Technol. 17(5) , 583-93, (2012)

Sustained release matrix pellets of the freely water soluble drug, betahistine dihydrochloride (BH), were prepared using freeze pelletization technique. Different waxes and lipids (cetyl alcohol, bees...

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...

 Synonyms

MFCD00012813
N-Methyl-2-(2-pyridinyl)ethanamine dihydrochloride
N-methyl-2-(pyridin-2-yl)ethanamine dihydrochloride
2-Pyridineethanamine, N-methyl-, hydrochloride (1:2)
Betahistine Hydrochloride
N-Methyl-2-pyridineethanamine Dihydrochloride
N-methyl-2-pyridin-2-ylethanamine,dihydrochloride
EINECS 226-966-5
Betahistine (dihydrochloride)
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