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CAS No.: 3978-86-7

Azatadine dimaleate/马来酸阿扎他定 Catalog No. CSN10364

Synonyms: Azatadine maleate;SCH 10649;Optimine

Azatadine dimaleate is an inhibitor of histamine and cholinergic with IC50 of 6.5 nM and 10 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 cholinergic

IC50:10nM Histamine Receptor

IC50:6.5nM
描述Azatadine Dimaleateis an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice^[3]. Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a Cmax of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation, demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine (8.8 mg oral) in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%^[4]. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9137 mL
- 9.5685 mL
- 19.1371 mL
- 5 mM
- 0.3827 mL
- 1.9137 mL
- 3.8274 mL
- 10 mM
- 0.1914 mL
- 0.9569 mL
- 1.9137 mL

技术信息

CAS号

3978-86-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H30N2O8

运输

蓝冰

分子量

522.55

别名

Azatadine maleate;SCH 10649;Optimine;Azatadine (maleate);azatadine;Idulamine;Idulian;Juste brand of azatadine maleate;Key brand of azatadine maleate;Lergocil;Schering brand of azatadine maleate;Schering-Plough brand of azatadine maleate;Zadine;马来酸阿扎他定

溶解度

DMSO	105.0 mg/mL (200.9 mM)
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
cholinergic		IC50:10nM
Histamine Receptor		IC50:6.5nM

Azatadine dimaleate/马来酸阿扎他定 Catalog No. CSN10364

靶点选择性

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