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CAS No.: 29608-49-9

Almitrine Bismesylate/二甲磺酸阿米三嗪 Catalog No. CSN21132

Synonyms: Almitrine bismesylate;Almitrine bismethanesulfonate;Almitrine dimesylate

Almitrine mesylate is an agonist of peripheral chemoreceptor and inhibits selectively the Ca2+-dependent K+ channel. It can improve chronic obstructive pulmonary disease and nocturnal oxygen desaturation.

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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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4931 mL
- 7.4654 mL
- 14.9307 mL
- 5 mM
- 0.2986 mL
- 1.4931 mL
- 2.9861 mL
- 10 mM
- 0.1493 mL
- 0.7465 mL
- 1.4931 mL

技术信息

CAS号

29608-49-9

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H37F2N7O6S2

运输

蓝冰

分子量

669.76

别名

Almitrine bismesylate;Almitrine bismethanesulfonate;Almitrine dimesylate;Vectarion;Almitrin;Almitrina;Almitrinum;Almitrine

溶解度

DMSO	98.0 mg/mL (146.3 mM)
Water	Insoluble
Ethanol	100.0 mg/mL (149.3 mM)

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Almitrine Bismesylate/二甲磺酸阿米三嗪 Catalog No. CSN21132

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