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29608-49-9

中文名称 甲磺酸阿米三嗪
英文名称 Almitrine dimesylate
CAS 29608-49-9
分子式 C28H37F2N7O6S2
分子量 669.76
MOL 文件 29608-49-9.mol
更新日期 2024/04/28 11:49:27
29608-49-9 结构式 29608-49-9 结构式

基本信息

中文别名
二甲基阿咪三嗪
甲磺酸阿米三嗪
二甲磺酸阿米三嗪(标准品)
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
英文别名
Mesylate AlMitrine
ALMITRINE DIMESILATE
ALMITRINE DIMESYLATE
ALMITRINE BISMESYLATE
Almitrine bismethanesulfonate
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
N2,N4-Diallyl-6-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1,3,5-triazine-2,4-diamine dimethanesulfonate
1,3,5-Triazine-2,4-diamine,6-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-N,N'-di-2-propenyl-,dimethanesulfonate
所属类别
原料药

物理化学性质

熔点243° (dec)
储存条件Sealed in dry,Room Temperature
溶解度可溶于氯仿(少许)、甲醇(少许)
形态固体
颜色白色

安全数据

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

常见问题列表

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.

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