A rate of hemorrhage accounted for 31 mg/kg in 80 adult dogs premedicated with promedol and atropine. After circular-hemic hypoxia caused by the hemorrhage, single intravenous administration of gutimine (35-40 mg/kg) transformed the carbohydrate metabolism in heart muscle: activated glycolysis and accelerated the rate of its products oxidation, maintained the free amino acids concentration at the level similar to that of intact animals, reduced the rate of creatine phosphate synthesis.
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Bioorg Med Chem Lett
January 2014
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, S.A.S. Nagar, Mohali 160062, Punjab, India. Electronic address:
A new class of compounds based on S-benzylated guanylthiourea has been designed as potential PfDHFR inhibitors using computer aided methods (molecular electrostatic potential, molecular docking). Several compounds in this class have been synthesized starting from guanylthiourea and alkyl bromides. In vitro studies showed that two compounds from this class are active with the IC50 value of 100 μM and 400 nM.
View Article and Find Full Text PDFBull Exp Biol Med
July 2012
Department of Pharmacology, SM Kirov Military Medical Academy, St. Petersburg, Russia.
Pronounced antihypoxic and antioxidant effects of preventive injection of succinic acid, aminothiol antihypoxants gutimine and amtizol, and succinate-containing aminothiol antihypoxants gutimine succinate and amtizol succinate to Wistar rats with acute hypoxic hypoxia have been demonstrated. Exogenous succinic acid was inferior to aminothiol compounds by antihypoxic effect, but superior to them by its effect on the level of LPO products. Succinate in the aminothiol molecule modulated the intensity of their antihypoxic and antioxidant effects.
View Article and Find Full Text PDFEksp Klin Farmakol
November 2009
The antihypoxic activity of six aminothiol and triazinoindole derivatives was studied on a model of hypobaric (hypoxic) hypoxia in rats. With respect to the antihypoxic activity, the compounds can be arranged in the following order: amtizole succinate = amtizole approximately equal to gutimine > T-475 > gutimine > succinate succinate. One of the possible mechanisms of action for all antyhypoxants is the inhibition of lipid peroxidation and recovery of hypoxia-induced antioxidant defense system in the brain, kidneys, liver, myocardium, and muscles, which results in reduction of the contents of malonic dialdehyde and lipid hydroperoxides and an increase in the activity of superoxide dismutase and the content of recovered glutathione.
View Article and Find Full Text PDFLipid peroxidation and antioxidant defense processes have been studied over the course of experimental Pseudomonas aeruginosa intoxication in albino rats injected with a lethal dose of exotoxin A. The development of intoxication is associated with intensification of lipid peroxidation, manifested by accumulation of malonic dialdehyde and diene conjugates and decreased peroxide resistance of erythrocytes. Superoxide dismutase and catalase activities were inhibited and the concentration of vitamin B dropped.
View Article and Find Full Text PDFEksp Klin Farmakol
November 1998
Department of Pharmacology, Lugansk State Medical University, Ukraine.
The survey deals with the up-to-date information in the literature on the problem of pharmacological correction of pathological changes found in the organism in the hypoxic syndrome. The principal approaches to pharmacotherapy of this pathological condition are pointed out. Information on the up-to-date and effective antihypoxia agents applied in medical practice and those in the stage of development is given.
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