Name | almitrine dimesylate |
---|---|
Synonyms |
S2620 bismethanesulfonate
ALMITRINE DIMESILATE 6-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}-N,N'-di(prop-2-en-1-yl)-1,3,5-triazine-2,4-diamine methanesulfonate (1:2) S 2620 bismethanesulfonate 1,3,5-Triazine-2,4-diamine, 6-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-N,N-di-2-propen-1-yl-, methanesulfonate (1:2) N,N'-Diallyl-6-{4-[bis(4-fluorophenyl)methyl]-1-piperazinyl}-1,3,5-triazine-2,4-diamine methanesulfonate (1:2) ALMITRINE BISMESYLATE Almitrine dimethanesulfonate Almitrine mesylate N,N'-Diallyl-6-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}-1,3,5-triazine-2,4-diamine methanesulfonate (1:2) 1,3,5-Triazine-2,4-diamine, 6-(4-(bis(4-fluorophenyl)methyl)-1-piperazinyl)-N,N'-di-2-propenyl-, dimethanesulfonate N,N'-Diallyl-6-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1,3,5-triazine-2,4-diamine dimethanesulphonate n,n'-diallyl-6-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1,3,5-triazine-2,4-diamine dimethanesulphonate 2,4-bis(allylamino)-6-[4-[bis(p-fluorophenyl)methyl]-1-piperazinyl]-s-triazine dimethanesulfonate Almitrine dimesylate |
Description | Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel. |
---|---|
Related Catalog | |
Target |
K+ channel[1] |
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]. |
Animal Admin | 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]. |
References |
Boiling Point | 606.2ºC at 760 mmHg |
---|---|
Molecular Formula | C28H37F2N7O6S2 |
Molecular Weight | 669.763 |
Exact Mass | 669.221497 |
PSA | 194.71000 |
LogP | 5.57570 |
Vapour Pressure | 1.21E-14mmHg at 25°C |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|