[Neuroprotective effect of cerebrocurin in a model of acute cerebral stroke].

Chronic administration of cerebrocurin and cerebrolysin to Mongolian jirds with acute cerebral stroke model led to a decrease in the mitochondrial dysfunction on the 4th day, which was manifested by their ability to inhibit the mitochondrial permeability transition pore opening, normalize the energy metabolism, and enhance c-fos gene expression. In addition, cerebrocurin restored the morphofunctional state of neurons and favored the cell loss mechanism switching from necrosis to apoptosis. With respect to all characteristics under consideration, the effect of cerebrocurin exceeded with statistical confidence that of cerebrolysin.

[Pharmacological correction of neuronal damage in sensomotor zone of frontal cortex under conditions of experimental cerebral blood flow pathology].

The administration of thiotriazoline, emoxypine and magnelong (a combined glycine-magnesium preparation) to animals with acute cerebral circulatory insufficiency showed significant neuroprotective effect in both acute and late ischemic periods, as indicated by the indices of cell density and number and the characteristics of apoptic and destructed neurons approaching those in the group of intact rats. Pyracetam showed cerebroprotective effect only in late ischemic period. Magnelong exhibited the most significant neuroprotective effect, maintaining cell density on the intact control level and reducing the number of apoptotic and destructed neurons.

[Pharmacological neuroprotection against experimental acute cerebral ischemia of neurons of sensomotor area of frontal cortex and hippocampus in rats].

Emoxypine, thiotriazoline, and NN-103 (a 4-hydrazinoquinasoline derivative) exhibit a pronounced neuroprotective action during acute cerebral stroke. Emoxypine and thiotriazoline are more effective in inhibiting death of neurons in the sensomotor area of the frontal cortex, while NN-103 is more active in the hippocampus. The ischemic death of neurons in the sensomotors area of the frontal cortex with equal probability takes place by karyopyknosis or cytolysis, while in the hippocampus, mainly by cytolysis. All preparations (except for piracetam) with antioxidants properties are powerful membranoprotective agents, which is confirmed by a considerable decrease in the rate of cytolysis both in the cortex and in the hippocampus. The use of piracetam in the case of acute cerebral stroke increases the rate of neuronal death in various areas of the cortex, up to complete destruction of nerve tissues with the formation of cysts (in hippocampus). The tested preparations exhibit different mechanism of neuroprotection: emoxypine and NN-103 (in the sensomotor area of the frontal cortex and hippocampus) and thiotriazoline (in the hippocampus) produce the neuroprotection action on the background of increased activity of transmissions and transcription processes, while thiotriazoline (in the sensomotor area of the frontal cortex) offers neuroprotection on the background of inhibited transcription and transmission activity.

[The antioxidant activity of S-(4-quinazolyl)mercaptoacetic acid benzylidene hydrazides in vitro in the "nitrosation stress" model]. / Izuchenie antioksidantnoi aktivnosti benzilidengidrazidov S-(4-khinazolil)merkaptouksusnoi kisloty na modeli "nitroziruiushchego stressa" in vitro.

The "nitrozation stress" causes modification of the antioxidant enzymes leading to a decrease in their activity. A decrease in this activity and the resulting increase in the production of OH* and NO2* radicals via ONOO* decomposition leads to a significant increase in the extent of free-radical peroxidation during the "nitrozation stress". These factors are unfavorable from the standpoint of oxidative phosphorylation, which is manifested by inhibited activity of the oxidative enzymes. S-(4-Quinazolyl)mercaptoacetic acid benzylidene hydrazides exhibit a high antiradical activity related to the presence of a mercapto group in the quinazoline fragment. The activity depends on the position of this group on and the number of substituents in the benzylidene fragment. The compounds studied reduce the extent of damage in the brain homogenates of rats under conditions of nitrozation stress. This is manifested by inhibition of the free-radical peroxidation and an increase in the activity of antioxidant and prooxidant enzymes.

[A comparison of the clinical efficacy of enalapril maleate analogs in patients with heart failure and ischemic heart disease]. / Sopostavlenie klinicheskoi éffektivnosti analogov énalaprila maleata u bol'nykh serdechnoi nedostatochnost'iu s ishemicheskoi bolezn'iu serdtsa.

The authors examined 68 patients aged from 42 to 68 years with ischemic heart disease without a history of myocardial infarction and with angina pectoris of exertion functional class 2-3 and circulatory insufficiency class 2 (according to NYHA criteria). The criteria serving as the reason for relating patients to the follow-up group were left-ventricular end-diastolic volume > 160 ml, ejection fraction < 30%, cardiothoracic index > 0.55, threshold power of endured loads within a range of 71.5 +/- 2.30 watt. After stabilization of the clinical status by means of basic therapy (nitrates, blockers of slow calcium channels, diuretics, antiaggregants), all patients were divided into two follow-up groups. The first group consisted of 36 patients who received renitec (10 mg/24 h), patients of group 2 were given enap in the same dose. The course of treatment lasted 12 weeks. The effectiveness of treatment was controlled by echocardiography according to the standard methods in M- and B-regimens. Analysis of the obtained data showed that within 12-day follow-up renitec demonstrated higher effectiveness and lesser incidence of side-effects than did enap given in the same dose.

[The optimization of the hemodynamic characteristics in patients with ischemic heart disease and circulatory failure by using a substrate-coenzyme complex]. / Optimizatsiia gemodinamicheskikh kharakteristik u bol'nykh ishemicheskoi bolezn'iu serdtsa s nedostatochnost'iu krovoobrashcheniia s pomoshch'iu substratno-kofermentnogo kompleksa.

On the basis of findings from evaluation of 65 patients with ischemic heart disease presenting with functional class II-III effort angina and FC II-III circulatory insufficiency (NYHA) a comparative assessment was carried out of efficacy of combined therapy involving basic antianginal agents and glucose-insulin-potassium mixture plus glutaminic acid versus solitary basic therapy. It has been shown that combined versus basic therapy is much more capable of restoring cardiohemodynamic interrelations. This was evidenced by a significant reduction of the postexercise level, improvement in the coordination of work of the arterial system, and augmentation of the left ventricular inotropic function.

[The use of the new cardioprotective agent thiotriazoline in the therapy of ischemic heart disease in older patients]. / Primenenie novogo kardioprotektornogo sredstva tiotriazolina v terapii ishemicheskoi bolezni serdtsa u lits starshego vozrasta.

The effect of tiotriazolin on the efficiency of antianginal therapy in aged patients with cardiac disease CD is studied. Clinical tests, functional (ECG, electrocardiotopography, cardiohemodynamics, etc.) and biochemical (indices of lipid peroxidation activity) methods of control were used as criteria of the treatment efficiency. Tiotriazolin was found to increase significantly the efficiency of basic drugs for CD treatment in aged patients.

[Antiradical and antioxidant activity of derivatives of 1,2,4-triazole and quinazoline in cerebral ischemia]. / Antiradikal'naia i antiokislitel'naia aktivnost' proizvodnykh 1,2,4-triazola i khinazolina pri ishemii golovnogo mozga.

Antioxidant and antiradical activity of 1,2,4-triazole and quinazoline derivatives inhibiting superradical at the initial stages of free-radical oxidation have been studied in vitro by the method of Hara P, Mista, 1972. It is acceptable for the determination of antiradical and antioxidant activity of newly synthesized compounds.

[The side effects of drugs]. / Pobochnye deistviia lekarstvennykh sredstv.

59.4% of drugs allowed by current pharmaceutical nomenclature to be sold without prescriptions may cause side effects or have contraindications. Analgetics, spasmolytics, purgatives and non-steroidal anti-inflammatory drugs account for the bulk of side effects. 87% of over-the-counter drugs contain no information about possible adverse effects. Promoting awareness of the population of side effects of the drugs admitted to prescription-less sale should be considered as an urgent problem of pharmacy.

[Antioxidant activity of a new derivative of 4-hydrazinoquinazoline in experimental cerebral hypoxia]. / Antioksidantnaia aktivnost'novogo proizvodnogo 4-gidrazinokhinazolina pri éksperimental'noi gipoksii golovnogo mozga.

It is established that KS-79 compound possesses the high level of antioxidant activity and realizes its antioxidant effect at initial stages of free-radical hydrogen peroxide oxidation of lipids. Due to this ability it differs from the oxidants of direct-type action.

[The effect of sodium salicylate and phenobarbital on the anti-arrhythmia properties of novocainamide and acetylnovocainamide]. / Vliianie natriia salitsilata i fenobarbitala na antiaritmicheskie svoistva novokainamida i atsetilnovokainamida.

CaCl2 and aconitic models of arrhythmias were reproduced in experiments with rats. Sodium salicylate was found to decrease the preventive effect of ecetylnovocainamidum and increased the effect of novocainamidum on ECG changes. Sodium salicylate diminished the preventive effect of acetyl-novocainamidum by elevating myocardial Na+ concentrations, favoured the decrease in myocardial K+ levels, eliminated the preventive effects of novocainamide and acetylnovocainamide by altering myocardial energy metabolism in CaCl2-induced arrhythmia and improved the preventive effect of acetyl-novocainamide on these parameters in aconitic arrhythmia.

[Study of anti-ischemic action of carnitine chloride and its effects on the effectiveness of antianginal agents]. / Issledovanie protivoishemicheskogo deistviia karnitina khlorida i ego vliianiia na éffektivnost' antianginal'nykh sredstv.

The experiments with models of myocardial infarction established that carnitine chloride reduced the size of an ischemic zone, prevented oxidative metabolism, lowered ATP and creatine phosphate levels, inhibited lactate and free fatty acid accumulation in the ischemic myocardium. Carnitine chloride in combination with nitrong and isoptin increased the anti-ischemic potency of the former.

[The effect of metabolic agents on the antiarrhythmic activity of novocainamide and acetylnovocainamide]. / Vliianie metaboliticheskikh sredstv na antiaritmicheskuiu aktivnost' novokainamida i atsetilnovokainamida.

The effects of potassium malate and sodium succinate on the antiarrhythmic activity of novocainamide and acetylnovocainamide during modelling of chlor-calcium-induced arrhythmia as well as in disorders of cardiac rhythm during modelling of pituitrin-isadrine-induced myocardial infarction were studied. The metabolic agents were found to increase the effectiveness of acetylnovocainamide and the toxicity of novocainamide. To interpret the specific features of the mechanism of the anti-arrhythmic action of the compounds there was studied their ability to form complexes with components of biomembranes and ions of biometals.

[The anti-arrhythmia activity of quinazopyrine]. / Issledovanie antiaritmicheskoi aktivnosti khinazopirina.

The antiarrhythmic activity of quinasopirine was studied in the experiments on rats with the use of models of calcium chloride- and aconitine-induced arrhythmias, disorders of cardiac rhythm in myocardial infarction produced by isadrine and pituitrin and also in the experiments on cats in arrhythmias caused by electric stimulation of the myocardium, postinfarction and reperfusion arrhythmias. Quinasopirine exhibits the antiarrhythmic effect being superior to that of anapriline and novocainamide in arrhythmias induced by calcium chloride and aconitine. In other types of the cardiac rhythm disorder its activity is comparable with that of ethmosine, obsidane and cordarone. Quinasopirine reduces automatism and contractile function of the myocardium.

[The mechanism of action of riboxin]. / K mekhanizmu deistviia riboksina.

The effect of riboxin (100 mg/kg body weight) on different kinds of metabolism in the cardiac muscles of Wistar rats in norm and during experimental pituitrin-neoepinephrine-induced myocardial infarction was studied. Riboxin was found to stimulate anaerobic glycolysis with the hyperproduction of lactate and the formation of glucose deficiency and also to increase the rate of protein synthesis on polyribosomes. Administration of riboxin during the formation of myocardial infarction considerably hinders the pronounced character of its electrocardiographic and biochemical manifestations. Thus, in the ischemic cardiac muscle the pool of macroergic phosphates is preserved, glycolysis and adaptive protein synthesis are impaired to a lesser degree that probably underlies the cardioprotective effect of riboxin.

[Effect of malic acid salts on physical work capacity and its recovery after exhausting muscular activity]. / Vliianie solei iablochnoi kisloty na fizicheskuiu rabotosposobnost' i ee vosstanovlenie posle istoshchaiushchei myshchechnoi deiatel'nosti.

The effect of malic acid salts of iron, potassium, copper, chromium, lithium and zinc on the motor activity and electroencephalographic indices in rats was studied under the course of oral treatment (250 mg/kg). Potassium malate was found to exert the most pronounced stimulating effect on the motor activity and excitatory processes in the sensory motor brain areas. The study of the influence of this compound on total physical working capacity and its restoration revealed a significant dose-dependent stimulating action. It was shown that the effects of potassium malate are related to its ability to stimulate the most productive bioenergetic processes, to increase carbohydrate reserves, to decrease oxygen consumption of tissues.

[Effect of quinazopyrine on the process of reparative regeneration]. / Vliianie khinazopirina na protsessy reparativnoi regeneratsii.

The effect of quinazopyrine on skin wound healing in rats was studied. Quinazopyrine was found to stimulate synthesis of nucleic acids, maturation of fibroblasts and to increase mechanical strength of the postoperative scar. This effect retains in animals with alloxan-induced diabetes. The wound-healing activity of quinazopyrine was higher than that of methyluracil, dimexide, pentoxyl, sodium nucleinate, potassium orotate and riboxine.

[Biological activity of the sum of the valepotriates isolated from Valeriana alliariifolia]. / Biologicheskaia aktivnost' summy valepotriatov, vydelennykh iz valeriany chesnochnikolistnoi.

The native sum of valepotriates isolated from Val. alliariifolia Adams which was named valiracyl is an agent of low toxicity and exerts a pronounced neurotropic effect. Valiracyl suppresses the orientation reflex of animals in an "open field", decreases a spontaneous and caffeine-stimulated motor activity, potentiates and prolongs the action of barbiturates, significantly reduces aggressiveness of animals, decreases sensitivity to the convulsant effects of corasol and thiosemicarbazide, produces the antihypoxic and mild myorelaxant actions. The neurotropic effects of valiracyl are related to increased level of the GABA inhibition mediator and decreased intensity of bioenergetic processes in the brain.