Betahistine Dihydrochloride

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

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].

Name	Betahistine dihydrochloride
Synonym	More Synonyms

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	Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Neurological Disease
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.

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

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.

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

Betahistine Dihydrochloride MSDS(Chinese)

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

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%

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...

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)