New Fluorine-Containing Openers of ATP-sensitive Potassium Channels Flocalin and Tioflocalin Inhibit Calcium-Induced Mitochondrial Pore Opening in Rat Hearts

Strutynska, Nataliya A.; Strutynskyi, Ruslan B.; Chorna, Snizhana V.; Semenykhina, Olena M.; Mys, Lidiya A.; Oo, Moĭbenko; Сагач, В. Ф.

doi:10.1615/intjphyspathophys.v5.i4.60

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“…The direct evidence of potassium channels opening with flocalin (which is a fluorine containing analogue of pinacidil [20]) is the result of the studies with the use of specific inhibitors of K ATP channels [21,22]. Owing to thorough experimental investigations cardioprotector flocalin is positioned primarily as a selective activator of K ATP channels [2,11,[20][21][22][23]. It has also been stated that flocalin inhibits sodium and Ca 2+ channels of L-type in cardiomyocytes [23].…”

Section: T a B L E 2 The Changes Of Fibrinolytic Activity Of Kidney mentioning

confidence: 99%

The experimental investigation of fibrinolytic system under the influence of flocalin in conditions of acute hypoxic kidney injury

Гоженко¹,

Gubsky²,

Filipets³

et al. 2017

Ukr.Biochem.J.

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in the experiments on rats subjected to acute hypoxic histochemical nephropathy, caused by sodium nitrite and 2,4-dinitrophenol, fibrinolytic activities of blood plasma, urine, renal cortex, medulla, and T he essential biochemical characteristic of plasma membranes ATP-sensitive potassium (K ATP ) channels, which are gated by intracellular nucleotides ATP and ADP, is their sensitivity to disturbances in cellular metabolism. Subsequently, rapid activation and opening of K ATP channels in response to the decrease of ATP level, in particular under conditions of ischemia and hypoxia, results in plasma membrane hyperpolarization and the decrease of voltage dependent inflow of Ca 2+ ions. The latter event is accompanied by drastic disturbance of energy metabolism compliance with the functional needs of the cell and initiates the pathological cascades leading to the profound cellular pathology.The regulatory role of K ATP channels in conditions of cellular oxygenation restriction was first studied on cardiomyocytes and smooth muscle cells of blood vessels [1], that resulted in the use of pharmacological activators of these channel types for treatment of cardiovascular diseases. In recent years the convincing evidence of cardioprotective and vasodilatory effects of the original K ATP channels fluoride-containing activator Flocalin -N-(-4-difluoromethoxyphenyl)-N′-1,2,2-trimethylpropyl-N′′-cyanoguanidine [2] were obtained. Owing to the presence of fluoride, flocalin is more selective to K ATP channels and less toxic compared to other representatives of potassium channels modulators that makes it perspective and promising pharmacological substance as physiological regulator and protector of metabolic processes disturbed under hypoxic and ischemic conditions.

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Section: T a B L E 2 The Changes Of Fibrinolytic Activity Of Kidney mentioning

confidence: 99%

The experimental investigation of fibrinolytic system under the influence of flocalin in conditions of acute hypoxic kidney injury

Гоженко¹,

Gubsky²,

Filipets³

et al. 2017

Ukr.Biochem.J.

View full text Add to dashboard Cite

show abstract

New Fluorine-Containing Openers of ATP-sensitive Potassium Channels Flocalin and Tioflocalin Inhibit Calcium-Induced Mitochondrial Pore Opening in Rat Hearts

Cited by 1 publication

References 0 publications

The experimental investigation of fibrinolytic system under the influence of flocalin in conditions of acute hypoxic kidney injury

The experimental investigation of fibrinolytic system under the influence of flocalin in conditions of acute hypoxic kidney injury

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