Almitrine dimesylate

Modify Date: 2024-01-02 19:43:12

Almitrine dimesylate Structure
Almitrine dimesylate structure
Common Name Almitrine dimesylate
CAS Number 29608-49-9 Molecular Weight 669.763
Density N/A Boiling Point 606.2ºC at 760 mmHg
Molecular Formula C28H37F2N7O6S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Almitrine dimesylate


Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.

 Names

Name almitrine dimesylate
Synonym More Synonyms

 Almitrine dimesylate Biological Activity

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

[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.

 Chemical & Physical Properties

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

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XY5850250
CHEMICAL 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
LAST UPDATED :
199112
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C26-H29-F2-N7.2C-H4-O3-S
MOLECULAR WEIGHT :
669.84

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 28,814,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
370 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JNPHAG Journal de Pharmacologie. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1970- Volume(issue)/page/year: 3,363,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
207 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JNPHAG Journal de Pharmacologie. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1970- Volume(issue)/page/year: 3,363,1972

 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
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