生物活性 | |||
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描述 | Flindokalner ,also known as BMS-204352, is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel isoforms expressed in HEK293 cells. Flindokalner is also a BKca-positive modulator. Flindokalner has a negative regulatory activity (Ki=3.0) on Kv7.1 channels. Flindokalner has negative modulatory activity on Kv7.1 channels (Ki=3.7 μM) and acts as a negative modulator of GABAA receptors. Flindokalner has anxiolytic efficacy in vivo[1][2].At a concentration of 10 μM, Flindokalner inhibits Kv7.4 and Kv7.5 with Ki values of 230 μM and 605 μM, respectively[1].In the concentration range of 1-10 μM, Flindokalner inhibited Ca2+ currents in a dose-dependent manner with a Kd value of 6 μM and a Hill coefficient of 1.33. In freshly isolated rat ventricular myocytes, Flindokalner inhibited cardiac L-type Ca2+ channels in a direct manner without affecting BKCa channels or intracellular signaling[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.78mL 0.56mL 0.28mL |
13.90mL 2.78mL 1.39mL |
27.80mL 5.56mL 2.78mL |
参考文献 |
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