Betahistine 2HCl

製品コードS3176 バッチS317602

印刷

化学情報

 Chemical Structure Synonyms PT-9 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C8H12N2.2HCl

分子量 209.12 CAS No. 5579-84-0
Solubility (25°C)* 体外 DMSO 38 mg/mL (181.71 mM)
Water 38 mg/mL (181.71 mM)
Ethanol 38 mg/mL (181.71 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
in vitro 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. [1]
in vivo Betahistine (< 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. [1] 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. [2] Betahistine-dihydrochloride (16 mg tid and 48 mg tid) shows that the number of attacks per month decreased in both doses over time in Meni鑢e's disease. [3] 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. [4]

プロトコル(参考用のみ)

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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