Flindokalner 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。

Flindokalner is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner displays a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM) and acts as a negative modulator of GABAA receptors and it also shows anxiolytic efficacy in vivo.

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].

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].

187523-35-9

C16H10ClF4NO2

359.7

BMS-204352;Flindokalner

DMSO:100 mg/mL (278.01 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years