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Betahistine

(Synonyms: 倍他司汀；培他啶)

目录号: PL14975 纯度: ≥98%

Betahistine 是一种具有口服活性的的组胺 H1 受体 (histamine H1 receptor) 激动剂和 H3 受体 (H3 receptor) 的拮抗剂。Betahistine 可以用于类风湿性关节炎 (RA) 的研究。

CAS No. :5638-76-6

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中文名称	Betahistine
中文别名	抗眩啶;倍他司汀;2-(2-甲氨基乙基)吡啶;N-甲基-N-2-（2-吡啶基）胺;倍他司汀杂质;2-(2-甲基氨基乙基)吡啶;N-甲基-2-吡啶乙胺
英文名称	Betahistine
英文别名	N-Methyl-2-(pyridin-2-yl)ethanamine;2-(2-Methylaminoethyl)pyridine;2-(Methylaminoethyl)pyridine;2-[2-(METHYLAMINO)ETHYL]PYRIDINE;Betahistine;N-methyl-2-pyridin-2-ylethanamine;N-Methyl-N-(2-pyridin-2-ylethyl)amine;N-Methyl-N-[2-(2-pyridyl)ethyl]amine;N-[2-(2-Pyridyl)ethyl]-N-methylamine;NSC 42617;OBE 101;Y-G 14;[2-(2-Pyridyl)ethyl]methylamine;beta-Histine
Cas No.	5638-76-6
分子式	C₈H₁₂N₂
分子量	136.19
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	Betahistine 是一种具有口服活性的的组胺 H1 受体 (histamine H1 receptor) 激动剂和 H3 受体 (H3 receptor) 的拮抗剂。Betahistine 可以用于类风湿性关节炎 (RA) 的研究。

产品详情

生物活性

Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).

性状

Liquid

IC50 & Target[1][2]

H1 Receptor H3 receptor

体外研究(In Vitro)

Betahistine (0-10 μM) inhibits [I]iodoproxyfan binding to membranes of CHO (rH3(445)R) and CHO (hH3(445)R) cells with IC50 values of 1.9 μM and 3.3 μM, respectively. Lead to Ki values of 1.4 μM and 2.5 μM, respectively.
Betahistine (0-10 μM) has a regulating function on cAMP formation in CHO (rH3(445)R), CHO (rH3(413)R), and CHO (hH3(445)R) cells. At low concentrations, betahistine behaves an apparent inverse agonist, and progressively enhances cAMP formation with EC50 values of 0.1 nM, 0.05 nM and 0.3 nM, respectively. In contrast, at concentrations higher than 10 nM, betahistine inhibits cAMP formation with an EC50 value of 0.1 μM in CHO (rH3(445)R) and full agonist activity.
has not independentl

体内研究(In Vivo)

Betahistine (intraperitoneal or oral administration; 0.1-30 mg/kg; single dose) with acute administration has increased tele-methylhistamine (t-MeHA) levels with an ED 50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED 50 of 2 mg/kg in male Swissmice.
Betahistine (oral adminstration; 1 and 5 mg/kg; daily for 3 weeks) attenuates the severity of arthritis and reduces the levels of pro-inflammatory cytokines in the paw tissues of CIA mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Poyurovsky M, et al. The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3.
[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 Sep 1;334(3):945-54.

溶解度数据	In Vitro: DMSO : 100 mg/mL (734.27 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Betahistine

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