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5579-84-0

5579-84-0 structure
5579-84-0 structure
  • Name: Betahistine Dihydrochloride
  • Chemical Name: Betahistine dihydrochloride
  • CAS Number: 5579-84-0
  • Molecular Formula: C8H14Cl2N2
  • Molecular Weight: 209.116
  • Catalog: API Circulatory system medication Peripheral vasodilator
  • Create Date: 2018-06-02 08:00:00
  • Modify Date: 2024-01-02 13:22:47
  • 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
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)
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.

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
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%