Azatadine dimaleate
产品说明书
 |
同义名 : | 二马来酸氮杂他定 ;Azatadine maleate; Azatadine (maleate); Zadine; Schering-Plough brand of azatadine maleate; Schering brand of azatadine maleate; Optimine; Lergocil; Key brand of azatadine maleate; Juste brand of azatadine maleate; Idulian; Idulamine; azatadine |
| CAS号 : | 3978-86-7 | |
| 货号 : | A550669 | |
| 分子式 : | C28H30N2O8 | |
| 纯度 : | 98% | |
| 分子量 : | 522.55 | |
| MDL号 : | MFCD00242593 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.91mL 0.38mL 0.19mL |
9.57mL 1.91mL 0.96mL |
19.14mL 3.83mL 1.91mL |
| 参考文献 |
|---|