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  • Azatadine dimaleate

    • 马来酸阿扎他定;Azatadine maleate
    货号: abs813496
    CAS号: 3978-86-7
    分子式: C20H22N2.2C4H4O4
    分子量: 522.55
    产品说明书
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    货号-规格 货期 价格 数量
    abs813496-10mg 1-2周 ¥604.00
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    abs813496-20mg 1-2周 ¥948.00
    - +
    abs813496-50mg 1-2周 ¥1654.00
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    abs813496-100mg 1-2周 ¥1892.00
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    大包装询价
    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.
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    • 实验方法 实验条件
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