Flindokalner, also known BMS-204352, is a neuroprotectant. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors.
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].
Flindokalner 动物研究
Animal study
Flindokalner induces dose-dependent anxiolytic effects in animals when administered intraperitoneally at doses of 3-30 mg/kg[1].
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