Almitrine Bismesylate

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Chemical Structure| 29608-49-9 同义名 : 甲磺酸阿米三嗪 ;Almitrine dimesylate; Almitrine bismethanesulfonate; Almitrine dimethanesulfonate; Almitrine mesylate
CAS号 : 29608-49-9
货号 : A242169
分子式 : C28H37F2N7O6S2
纯度 : 98%+
分子量 : 669.76
MDL号 : MFCD01679060
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
生物活性
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
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

[1]López-López JR, Pérez-García MT, Canet E, Gonzalez C. Effects of almitrine bismesylate on the ionic currents of chemoreceptor cells from the carotid body. Mol Pharmacol. 1998;53(2):330-339

[2]Bee D, Emery CJ, Howard P. An analysis of the action of an analogue of almitrine bismesylate in the rat model of hypoxic lung disease. Exp Physiol. 1992;77(6):819-828