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  • Asimadoline

    • 阿西马朵林;EMD-61753
    货号: abs820907
    CAS号: 153205-46-0
    分子式: C27H30N2O2
    分子量: 414.54
    产品说明书
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    货号-规格 货期 价格 数量
    abs820907-5mg 4周 ¥1120.00
    - +
    abs820907-25mg 4周 ¥4484.00
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    大包装询价
    产品描述
    描述
    Asimadoline is a potent κ opioid receptor agonist with IC50s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.
    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
    阿西马朵林;EMD-61753
    可溶性/溶解性
    DMSO : ≥ 103.3 mg/mL (249.19 mM)
    生物活性
    In vitro(体外研究)
    The IC50 for Asimadoline binding to μ-opioid receptors is 3 µM and to δ-opioid receptors is 0.7 µM. The IC50 values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 IC50, suggesting no relevant antihistaminergic, antiserotonergic or anticholinergic effects. At high concentrations, Asimadoline demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC50=4.2 µM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.
    In vivo(体内研究)
    Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats[3]. The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels.
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    • 实验方法 实验条件
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