1. Materials information
Names
| Name | almitrine dimesylate |
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| Synonym | More Synonyms |
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Almitrine dimesylate Biological Activity
| Description | Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel. |
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| Related Catalog | Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Research Areas >> Cardiovascular Disease Research Areas >> Neurological Disease |
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| Target | K+ channel[1] |
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| 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]. |
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| 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]. |
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| 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]. |
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| References | [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. |
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Chemical & Physical Properties
| Boiling Point | 606.2ºC at 760 mmHg |
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| Molecular Formula | C28H37F2N7O6S2 |
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| Molecular Weight | 669.763 |
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| Exact Mass | 669.221497 |
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| PSA | 194.71000 |
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| LogP | 5.57570 |
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| Vapour Pressure | 1.21E-14mmHg at 25°C |
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Toxicological Information
CHEMICAL IDENTIFICATIONCHEMICAL NAME : 1,3,5-Triazine-2,4-diamine, 6-(4-(bis(4-fluorophenyl)methyl)-1-piperazinyl)-N,N'- di-2- propenyl-, dimethanesulfonate
CAS REGISTRY NUMBER : 29608-49-9
MOLECULAR FORMULA : C26-H29-F2-N7.2C-H4-O3-S
HEALTH HAZARD DATAACUTE TOXICITY DATASPECIES OBSERVED : Rodent - mouse
REFERENCE : EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 28,814,1972
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
REFERENCE : JNPHAG Journal de Pharmacologie. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1970- Volume(issue)/page/year: 3,363,1972
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
REFERENCE : JNPHAG Journal de Pharmacologie. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1970- Volume(issue)/page/year: 3,363,1972
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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 |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
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