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/ 组胺受体 / Betahistine 2HCl

盐酸倍他司汀 /Betahistine 2HCl {[allProObj[0].p_purity_real_show]}

货号：A120842 同义名： N-甲基-2-吡啶乙胺二盐酸盐 / Betahistine (hydrochloride);PT-9 Ambeed 开学季，买赠积分，赢豪礼

Betahistine 2HCl is histamine H3 receptor inhibitor with IC50 of 1.9 μM. It is an antivertigo drug.

Betahistine 2HCl 化学结构 CAS号：5579-84-0
Betahistine 2HCl 化学结构
CAS号：5579-84-0
Betahistine 2HCl 3D分子结构
CAS号：5579-84-0
Betahistine 2HCl 化学结构 CAS号：5579-84-0
Betahistine 2HCl 3D分子结构 CAS号：5579-84-0
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Betahistine 2HCl 纯度/质量文件 产品仅供科研

货号：A120842 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl {[allProObj[0].p_purity_real_show]}
Cyclizine ✔ {[allProObj[0].p_purity_real_show]}
Loratadine +

B(0)AT2, IC50: 4 μM

 		{[allProObj[0].p_purity_real_show]}
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		{[allProObj[0].p_purity_real_show]}
Doxylamine succinate ✔ {[allProObj[0].p_purity_real_show]}
Ebastine ✔ {[allProObj[0].p_purity_real_show]}
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		{[allProObj[0].p_purity_real_show]}
Meclizine dihydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		{[allProObj[0].p_purity_real_show]}
Diphenhydramine HCl ✔ {[allProObj[0].p_purity_real_show]}
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		{[allProObj[0].p_purity_real_show]}
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		{[allProObj[0].p_purity_real_show]}
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		{[allProObj[0].p_purity_real_show]}
Pemirolast potassium ✔ {[allProObj[0].p_purity_real_show]}
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		{[allProObj[0].p_purity_real_show]}
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		{[allProObj[0].p_purity_real_show]}
Brompheniramine maleate ✔ {[allProObj[0].p_purity_real_show]}
Carbinoxamine maleate salt ✔ {[allProObj[0].p_purity_real_show]}
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		{[allProObj[0].p_purity_real_show]}
Ketotifen fumarate salt ✔ {[allProObj[0].p_purity_real_show]}
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR {[allProObj[0].p_purity_real_show]}
Famotidine ✔ {[allProObj[0].p_purity_real_show]}
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		{[allProObj[0].p_purity_real_show]}
Lafutidine ✔ {[allProObj[0].p_purity_real_show]}
Cimetidine ✔ {[allProObj[0].p_purity_real_show]}
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE {[allProObj[0].p_purity_real_show]}
Ranitidine ✔ {[allProObj[0].p_purity_real_show]}
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		{[allProObj[0].p_purity_real_show]}
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		{[allProObj[0].p_purity_real_show]}
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

 		{[allProObj[0].p_purity_real_show]}
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		{[allProObj[0].p_purity_real_show]}
Azelastine HCl ✔ {[allProObj[0].p_purity_real_show]}
Epinastine HCl ✔ {[allProObj[0].p_purity_real_show]}
Levodropropizine ✔ {[allProObj[0].p_purity_real_show]}
Cyproheptadine hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Hesperetin ✔ {[allProObj[0].p_purity_real_show]}
Olopatadine HCl ✔ {[allProObj[0].p_purity_real_show]}
Mianserin hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Buclizine 2HCl ✔ {[allProObj[0].p_purity_real_show]}
Latrepirdine 2HCl ✔ GluR {[allProObj[0].p_purity_real_show]}
Cetirizine 2HCl ✔ {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Betahistine 2HCl 生物活性

描述 Betahistine dihydrochloride (BDH) is a histamine analog used to control weight gain, with short elimination half-life and gastric irritation as side effects. BDH ethosomal gel showed effective, sustained transdermal absorption and central action in decreasing food intake and, consequently, the weight gain[3]. BDH is systemically effective and well-tolerated when applied topically in hydrogel-based systems. The Carbopol-Poloxamer gel is a promising modality for transdermal delivery of BH[4]. BDH is widely used in relieving the symptoms associated with Ménière's syndrome. The obtained results suggest that betahistine-loaded chitosan microspheres prepared by solvent evaporation method are capable of sustained release of drugs and therefore can be used as drug delivery systems in the treatment of Ménière's syndrome[5].

Betahistine 2HCl 参考文献

[1]Gbahou F, Davenas E, 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.

[2]Mira E, Guidetti G, et al. Betahistine dihydrochloride in the treatment of peripheral vestibular vertigo. Eur Arch Otorhinolaryngol. 2003 Feb;260(2):73-7.

[3]El-Menshawe SF, Ali AA, Halawa AA, Srag El-Din AS. A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization. Drug Des Devel Ther. 2017 Nov 28;11:3377-3388

[4]Elkomy MH, El-Menshawe SF, Ali AA, Halawa AA, El-Din ASGS. Betahistine dihydrochloride transdermal delivery via optimized thermosensitive gels: percutaneous absorption evaluation using rat growth as a biomarker. Drug Deliv Transl Res. 2018 Feb;8(1):165-177

[5]Pilicheva BA, Kassarova MI, Zagorchev PI, Uzunova YI. Formulation and performance evaluation of betahistine dihydrochloride microspheres as sustained release systems. Folia Med (Plovdiv). 2014 Jul-Sep;56(3):187-93

Betahistine 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.78mL

0.96mL

0.48mL

23.91mL

4.78mL

2.39mL

47.82mL

9.56mL

4.78mL

Betahistine 2HCl 技术信息

CAS号5579-84-0
分子式C8H14Cl2N2
分子量 209.116
别名 N-甲基-2-吡啶乙胺二盐酸盐 ;Betahistine (hydrochloride);PT-9;Betahistine dihydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 35 mg/mL(167.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(239.1 mM)

DMF: 5 mg/mL(23.91 mM)，配合低频超声助溶
动物实验配方

Tags: Betahistine | 5579-84-0 | Histamine Receptor | antipsychotic | Histamine Receptor Modulator | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Betahistine 2HCl 纯度/质量文件 | Betahistine 2HCl 亚型比较 | Betahistine 2HCl 生物活性 | Betahistine 2HCl 参考文献 | Betahistine 2HCl 实验方案 | Betahistine 2HCl 技术信息

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