生物活性 | |||
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描述 | Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel. Almitrine at concentrations up to 10 mM did not affect whole-cell voltage-dependent K+, Ca2+, or Na+ currents in rat or rabbit cells. However, this concentration of almitrine significantly inhibited the Ca2+-dependent component of K+ currents in rat chemoreceptor cells. Almitrine inhibits the activity of a high-conductance (152±13 pS), Ca2+-dependent K+ channel by decreasing its open probability, with IC50 value of 0.22 μM. The inhibitory effect of almitrine on Ca2+-dependent K+ channels was also observed in GH3 cells[1]. 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[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.49mL 0.30mL 0.15mL |
7.47mL 1.49mL 0.75mL |
14.93mL 2.99mL 1.49mL |
参考文献 |
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