依来曲普坦氢溴酸盐 T0216

Product Introduction
Bioactivity


英文名: Eletriptan hydrobromide

描述: Eletriptan hydrobromide (Eletriptan HBr) 是一种口服活性激动剂，对 5-HT1B/1D 受体具有特异性亲和力，Ki 值分别为 0.92 和 3.14 nM。

体外活性: [3H]Eletriptan 与 5-HT1B 和 5-HT1D 的结合位点总数（Bmax）分别为 2478 fmol/mg 和 1576 fmol/mg。[3H]Eletriptan 的结合率（K(on) 0.249/min/nM）明显快于[3H]舒马曲坦（K(on) 0.024/min/nM），而脱落率（K(off) 0.027/min，而[3H]舒马曲坦为 0.037/min）则明显慢于[3H]Eletriptan 。[1] Eletriptan 可引起脑膜动脉、冠状动脉和隐静脉的浓度依赖性收缩。Eletriptan 在脑膜动脉中的效力高于冠状动脉（86 倍）或隐静脉（66 倍）。在临床试验中观察到的Eletriptan（40 mg和 80 mg）和舒马曲坦（100 mg）在脑膜动脉自由 C（最大值）时的预测收缩力相似。[2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 46.3 mg/mL (100 mM)


关键字: Inhibitor | Eletriptan Hydrobromide | Eletriptan hydrobromide | Eletriptan | 5-hydroxytryptamine Receptor | UK 116044 | 5-HT Receptor | UK116044 | inhibit | Serotonin Receptor

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途