Azatadine dimaleate
- 马来酸阿扎他定;Azatadine maleate
货号-规格 | 货期 | 价格 | 数量 |
abs813496-10mg | 1-2周 | ¥604.00 | - + |
abs813496-20mg | 1-2周 | ¥948.00 | - + |
abs813496-50mg | 1-2周 | ¥1654.00 | - + |
abs813496-100mg | 1-2周 | ¥1892.00 | - + |

产品描述 | ||
描述 | Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. Azatadine puts back 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. It 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. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | 马来酸阿扎他定;Azatadine maleate | |
外观 | 白色至淡奶油色粉末 | |
可溶性/溶解性 | DMSO :97 mg/mL (185.6 mM) Water :96 mg/mL (183.7 mM) | |
生物活性 | ||
靶点 | Histamine receptor,Cholinergic | |
In vitro(体外研究) | 95% of Azatadine is biotransformed in Sabouraud dextrose broth within 72 hours treatment with two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine. | |
In vivo(体内研究) | 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. 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%. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. | |
参考文献 | ||
参考文献 | The pharmacology of azatadine, a potential antiallergy drug. Tozzi S,et al. Agents Actions. 1974 Oct;4(4):264-70. PMID: 4155594. Comparati 䔸Żᩄ 族痛셌Ų 族痛셌Ų Item 褐 Count ๏ 趌๐ 侮靴 ᠠi S ñ ñ 眘⮦眀⮦敲痛๏ࠃ 馸鳘祖Item Ɲƞ Count 洣盜᬴叫㺍痭ᠠ靴i 縉 靴蘿敌ଧ靴ᠠi ᭰叫㺍痭ᡸ顴먲ନ魈 | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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