Name | N,N'-diallyl-6-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1,3,5-triazine-2,4-diamine dimethanesulphonate |
Synonyms | Mesylate AlMitrine ALMITRINE DIMESYLATE 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 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 6-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}-N,N'-diprop-2-en-1-yl-1,3,5-triazine-2,4-diamine dimethanesulfonate |
CAS | 29608-49-9 |
EINECS | 249-726-1 |
InChI | InChI=1/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) |
Molecular Formula | C28H37F2N7O6S2 |
Molar Mass | 669.76 |
Melting Point | 243° (dec) |
Boling Point | 606.2°C at 760 mmHg |
Flash Point | 320.4°C |
Solubility | Chloroform (Slightly), Methanol (Slightly) |
Vapor Presure | 1.21E-14mmHg at 25°C |
Appearance | Solid |
Color | White |
Storage Condition | Sealed in dry,Room Temperature |
In vitro study | 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. |
In vivo study | 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. |
Toxicity | LD50 in mice: 210 mg/kg i.v., 390 mg/kg i.p., >2 g/kg orally (Regnier) |
This product is 2, 4-bis (allylamino)-6-[4-bis-(p-fluorophenyl)] methyl]-L-piperazinyl-S-tricresyl-bis-methanesulfonate. The content of C26H29F2N7 • 2CH3S03H shall be 98.0% ~ 102.0% calculated as dry product.
take 0.50g of this product, add 50ml of water, shake for 10 minutes, filter, take the filtrate, according to the law (General 0631),pH value should be 2.0~3.5.
take this product about 35mg, precision weighing, according to the fluorine inspection method (General 0805) determination, fluorine content should be 5.1% ~ 6.3%.
take about 30mg of this product, put it in a 100ml measuring flask, add the mobile phase to dissolve and dilute to the scale, shake well, and use it as a test solution, set in a 100ml measuring flask and dilute to the scale with the mobile phase as a control solution. According to the chromatographic conditions under the content determination item, 20ul of the test solution and the control solution are accurately measured, and the human liquid chromatograph is injected respectively, and the chromatogram is recorded to 2 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution.
take this product, precision weighing, add dimethyl sulfoxide to dissolve and make a solution containing 20mg per 1ml, according to the residual solvent determination method (General 0861), the residual amount of toluene should be in accordance with the regulations.
take 0.50g of this product and add 25ml of ethanol to dissolve it. In addition to diluting it with ethanol, check it according to law (General rule 0801), and compare it with the control solution made of standard sodium chloride solution, no more concentrated (0.01%).
take 0.50g of this product, add 50ml of water, slowly boil for 2 minutes, let it cool, add additional water to the original volume, shake, filter, take 40ml of filtrate, inspection according to law (General rule 0802), compared with the standard potassium sulfate solution 0.05% ML made of control solution, should not be more concentrated ().
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.15%.
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
measured by high performance liquid chromatography (General 0512).
Central stimulant.
light shielding, sealed storage.
Biological activity | Almitrine mesylate is an agonist of peripheral chemoreceptors that selectively inhibits Ca2 +-dependent K channels. |
target | K channel |
category | toxic substances |
toxicity classification | highly toxic |
acute toxicity | oral administration-mouse LD50: 2000 mg/kg; Abdominal cavity-mouse LD50: 370 mg/kg |
flammability hazard characteristics | combustible; combustion produces toxic nitrogen oxides, sulfur oxides and fluoride smoke |
storage and transportation characteristics | warehouse ventilation and low temperature drying; separate from food raw materials |
fire extinguishing agent | dry powder, foam, sand, carbon dioxide, mist water |