Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca-dependent K channel.
IC50&Target
K channel
体外研究
Almitrine inhibits the activity of a high-conductance (152±13 pS), Ca-dependent K channel by decreasing its open probability. The IC50 value of the effect is 0.22 μM. The inhibitory effect of Almitrine on Ca-dependent K channels also is observed in GH3 cells. Almitrine at concentrations up to 10 μM does not affect whole-cell voltage-dependent K, Ca, or Na currents in rat or rabbit cells. However, this concentration of Almitrine significantly inhibits the Ca-dependent component of K currents in rat chemoreceptor cells.
体内研究
Almitrine acts via the peripheral arterial chemoreceptors raising carotid sinus nerve output and minute ventilation. Almitrine also has a pulmonary vascular action causing a dose-dependent constriction and dilatation. At low doses Almitrine enhances hypoxic pulmonary vasoconstriction and may improve the overall ventilation/perfusion ratio.
分子式
C28H37F2N7O6S2
分子量
669.76
CAS号
29608-49-9
中文名称
甲磺酸阿米三嗪;甲磺酸阿米替林
运输条件
Room temperature in continental US; may vary elsewhere.