化合物Flindokalner T15286

Product Introduction
Bioactivity


英文名: Flindokalner

描述: Flindokalner (BMS-204352) 是一种钾离子通道调节剂。它是大电导钙激活 K 通道正向调节剂。它是在 HEK293 细胞中表达的所有神经元 Kv7通道亚型的正调节剂。它在 Kv7.1 通道 (Ki=3.7 μM) 处显示负调节活性，并充当 GABAA 受体的负调节剂。它在体内显示出抗焦虑功效。

体外活性: Flindokalner inhibits cardiac L-type Ca2+ channels in a direct manner, without affecting BKCa channels or intracellular signal transduction, in freshly isolated rat ventricular myocytes. Flindokalner (10 μM) inhibits Kv7.4and Kv7.5 (Kis: 230 and 605 μM, respectively)[1]. Flindokalner (1-10 μM) causes inhibition of the Ca2+ current in a dose-dependent manner (Kd: 6 μM and a Hill coefficient: 1.33) [2].

体内活性: Flindokalner (3-60 mg/kg; i.p.) engenders an anxiolytic profile, in a shock-based conditioned model of anxiety in male Wistar rats. Flindokalner (3-30 mg/kg; i.p.) induces a dose-dependent anxiolytic effect [1].

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

溶解度: DMSO : 100 mg/mL (278.01 mM)


关键字: inhibit | KcsA | neuronal | ventricular | Flindokalner | effects | anxiolytic | BMS204352 | subtype | Potassium Channel | Inhibitor | myocytes | BMS 204352 | current

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相关库: Ion Channel Inhibitor Library | Potassium Channel Blocker Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | NO PAINS Compound Library | Bioactive Compound Library

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