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Betahistine 2HCl

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Chemical Structure| 5579-84-0 同义名 : N-甲基-2-吡啶乙胺二盐酸盐 ;Betahistine (hydrochloride);PT-9;Betahistine dihydrochloride
CAS号 : 5579-84-0
货号 : A120842
分子式 : C8H14Cl2N2
纯度 : 98%
分子量 : 209.116
MDL号 : MFCD00012813
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：
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].
实验方案
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
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