甲磺酸阿米三嗪

中文名称:

甲磺酸阿米三嗪

中文同义词:

N,N-二烯丙基-6-[4-[二(4-氟苯基)甲基]哌嗪-1-基]-1,3,5-三嗪-2,4-二胺二甲磺酸盐;甲磺酸阿米三嗪;二甲基阿咪三嗪;二甲磺酸阿米三嗪(标准品)

英文名称:

Almitrine dimesylate

英文同义词:

ALMITRINE BISMESYLATE;ALMITRINE DIMESYLATE;2,4-bis(allylamino)-6-[4-[bis(p-fluorophenyl)methyl]-1-piperazinyl]-s-triazine dimethanesulfonate;n,n-diallyl-6-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1,3,5-triazine-2,4-diamine dimethanesulphonate;ALMITRINE DIMESILATE;Mesylate AlMitrine;N2,N4-Diallyl-6-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1,3,5-triazine-2,4-diamine dimethanesulfonate;Almitrine bismethanesulfonate

CAS号:

29608-49-9

分子式:

C28H37F2N7O6S2

分子量:

669.76

EINECS号:

249-726-1

相关类别:

药物标准品;医药原料;医药中间体;标准品;中药对照品;原料药

Mol文件:

29608-49-9.mol

熔点 

243° (dec)

储存条件 

Sealed in dry,Room Temperature

生物活性

Almitrine mesylate 是一种外周化学感受器的激动剂，选择性抑制 Ca2+依赖性的 K+ 通道。

靶点

K + channel

体外研究

Almitrine inhibits the activity of a high-conductance (152±13 pS), Ca 2+ -dependent K + channel by decreasing its open probability. The IC 50 value of the effect is 0.22 μM. The inhibitory effect of Almitrine on Ca 2+ -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 2+ , or Na + currents in rat or rabbit cells. However, this concentration of Almitrine significantly inhibits the Ca 2+ -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.

类别

有毒物品

毒性分级

高毒

急性毒性

口服-小鼠 LD50: 2000 毫克/公斤; 腹腔-小鼠 LD50: 370 毫克/公斤

可燃性危险特性

可燃; 燃烧产生有毒氮氧化物, 硫氧化物和氟化物烟雾

储运特性

库房通风低温干燥; 与食品原料分开存放

灭火剂

干粉,泡沫,沙土,二氧化碳, 雾状水

毒性

LD50 in mice: 210 mg/kg i.v., 390 mg/kg i.p., >2 g/kg orally (Regnier)