Betahistine(Synonyms: 倍他司汀;培他啶)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Betahistine (Synonyms: 倍他司汀;培他啶) 纯度: ≥98.0%

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。

Betahistine(Synonyms: 倍他司汀;培他啶)

Betahistine Chemical Structure

CAS No. : 5638-76-6

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Betahistine 相关产品

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生物活性

Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine is used for the study of rheumatoid arthritis (RA)[3].

IC50 & Target[1]

H1 Receptor

 

H3 receptor

 

体外研究
(In Vitro)

Betahistine (0-10 μM) inhibits [125I]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[2].
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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 ED50 of 0.4 mg/kg, indicating the inverse agonism. Besides, after acute oral administration, it increases t-MeHA levels with an ED50 of 2 mg/kg in male Swissmice[2].
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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Collagen-induced arthritis (CIA) DBA/1 male mouse model[3]
Dosage: 1 mg/kg; 5mg/kg
Administration: Oral adminstration; day 21 to day 42 after a 21-day CIA induction
Result: Ameliorated mouse CIA by decreasing joint destruction.

Clinical Trial

分子量

136.19

Formula

C8H12N2

CAS 号

5638-76-6

中文名称

倍他司汀;培他啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (734.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.3427 mL 36.7134 mL 73.4268 mL
5 mM 1.4685 mL 7.3427 mL 14.6854 mL
10 mM 0.7343 mL 3.6713 mL 7.3427 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (18.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (18.36 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (18.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (18.36 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (18.36 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (18.36 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

    [3]. Tang KT, et al. Betahistine attenuates murine collagen-induced arthritis by suppressing both inflammatory and Th17 cell responses.Int Immunopharmacol. 2016 Oct;39:236-245.

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