CAS |
No.29608-49-9 |
中文名称 |
甲磺酸阿米三嗪 |
英文名称 |
Almitrine mesylate |
别名 |
Almitrinebismesylate;Teroxirone;二甲基阿咪三嗪;ALMITRINEBISMESYLATE;ALMITRINEDIMESYLATE; |
分子式 |
C28H37F2N7O6S2 |
分子量 |
669.76 |
溶解性 |
Soluble in DMSO ≥10mg/mL(Need ultrasonic) |
纯度 |
≥98% |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
MDL |
MFCD01679060 |
SMILES |
CS(=O)(=O)O.CS(=O)(=O)O.C=CCNC1=NC(=NC(=N1)N2CCN(CC2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F)NCC=C |
InChIKey |
MRDBGMJEPGXQHJ-UHFFFAOYSA-N |
InChI |
InChI=1S/C26H29F2N7.2CH4O3S/c1-3-13-29-24-31-25(30-14-4-2)33-26(32-24)35-17-15-34(16-18-35)23(19-5-9-21(27)10-6-19)20-7-11-22(28)12-8-20;2*1-5(2,3)4/h3-12,23H,1-2,13-18H2,(H2,29,30,31,32,33);2*1H3,(H,2,3,4) |
PubChem CID |
6918543 |
靶点 |
Potassium Channel |
通路 |
Membrane Transporter&Ion Channel |
背景说明 |
Almitrine mesylate 选择性抑制 Ca2+依赖性的 K+ 通道。 |
生物活性 |
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.[1-2] |
In Vitro |
Almitrine inhibits the activity of a high-conductance (152±13 pS), Ca2+-dependent K+ channel by decreasing its open probability. The IC50 value of the effect is 0.22 μM. The inhibitory effect of Almitrine on Ca2+-dependent K+ channels also is observed in GH3 cells. Almitrine at concentrations up to 10 μM does not affect whole-cell voltage-dependent K+, Ca2+, or Na+ currents in rat or rabbit cells. However, this concentration of Almitrine significantly inhibits the Ca2+-dependent component of K+ currents in rat chemoreceptor cells[1]. |
In Vivo |
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]. |
动物实验 |
Rats[2]8-week-old male spf Wistar rats are used. Rats are anaesthetized with Thiobarbiturate inactin (BYK, 100 mg/kg, i.p.). The interaction of the ventilatory response to hypoxia and an intermittent (2 min on, 1 min break) low-dose (10 μg/kg per min) and high-dose (80 μg/kg per min) infusion of S9581 or Almitrine is tested in control and chronically hypoxic rats. S9581 or Almitrine is infused intravenously (100 μg/ mL). Inspired oxygen levels were controlled by passing oxygen-nitrogen mixtures across the tracheal port at a flow rate of 3-41 min-1[2]. |
数据来源文献 |
[1]. López-López JR, et al. Effects of Almitrine bismesylate on the ionic currents of chemoreceptor cells from the carotid body. Mol Pharmacol. 1998 Feb;53(2):330-9. [2]. Bee D, et al. An analysis of the action of an analogue of Almitrine bismesylate in the rat model of hypoxic lung disease. Exp Physiol. 1992 Nov;77(6):819-28. |
规格 |
5mg 10mg 50mg 100mg |
单位 |
瓶 |