Almitrine dimesylate

Research use only, not for human use.

Almitrine dimesylate inhibits selectively the Ca2+-dependent K+ channel and that in rat chemoreceptor cellsused in the treatment of hypoxemic chronic lung diseases.

Almitrine dimesylate inhibits selectively the Ca2+-dependent K+ channel and that in rat chemoreceptor cellsused in the treatment of hypoxemic chronic lung diseases.(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.(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.

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.

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.

Almitrine mesylate | Almitrine bismesylate | Almitrine bismethanesulfonate

Cell Cycle/DNA Damage

Potassium Channel

Potassium Channel

Metabolic Disease

chronic obstructive pulmonary disease

29608-49-9

669.76

C28H37F2N7O6S2

>98% (HPLC)

DMSO:125 mg/mL (186.63 mM)

CS(O)(=O)=O.CS(O)(=O)=O.Fc1ccc(cc1)C(N1CCN(CC1)c1nc(NCC=C)nc(NCC=C)n1)c1ccc(F)cc1

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(-20℃)

With Ice Pack

≥ 2 years