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Betahistine 2HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Betahistine 2HCl图片
CAS NO:5579-84-0
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议
25g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)209.12
FormulaC8H12N2.2HCl
CAS No.5579-84-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 38 mg/mL (181.7 mM)
Water: 38 mg/mL (181.7 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)

Chemical Name: Methyl[2-(2-pyridyl)ethyl]amine dihydrochloride

SMILES Code: CNCCC1=NC=CC=C1.[H]Cl.[H]Cl

SynonymsPT-9; Betahistine dihydrochloride; Betahistine HCl; PT 9; PT9; trade names Veserc, Serc, Hiserk, Betaserc, Vergo.
实验参考方法
In Vitro

In vitro activity: Betahistine progressively enhances cAMP formation with a maximal effect, observed up to 10 nM, in CHO(H3R) cells incubated with 3 μM forskolin. In contrast, at concentrations higher than 10 nM betahistine progressively inhibits cAMP formation in CHO(H3R) cells incubated with 3 μM forskolin. Betahistine progressively reduces A23187-evoked [3H]arachidonic acid release (EC50=0.1 nM) with a maximal effect, observed up to 30 nM A23187-evoked [3H]arachidonic acid release from CHO(H3R) cells. Betahistine progressively enhanced the release of A23187-evoked [3H]arachidonic acid from CHO(H3R) cells at concentrations higher than 30 NM.

In VivoBetahistine (< 30 mg/kg) increases t-MeHA levels in a dose-dependent manner with an ED50 of 2 mg/kg and a maximal effect of ~35% reached at 30 mg/kg in mouse brain. Betahistine (16 mg twice per day for 3 months) has a significant effect on the frequency, intensity and duration of vertigo attacks, associated symptoms and the quality of life also are significantly improved in patients with Meniere's disease. Betahistine-dihydrochloride (16 mg tid and 48 mg tid) shows that the number of attacks per month decreased in both doses over time in Meniere's disease. Betahistine (50 mg/kg) treatment induces symmetrical changes with up-regulation of histidine decarboxylase mRNA in the tuberomammillary nucleus and reduction of [3H]N-alpha-methylhistamine labeling in both the tuberomammillary nucleus, the vestibular nuclei complex and nuclei of the inferior olive in brain sections of cats.
Animal modelMice
Formulation & Dosage30 mg/kg
References

J Pharmacol Exp Ther. 2010 Sep 1;334(3):945-54; Eur Arch Otorhinolaryngol. 2003 Feb;260(2):73-7.