[The action of bemitil on the self-regulation systems during short-term immobilization]. / Deistvie bemitila na sostoianie sistem samoreguliatsii pri kratkovremennoi immobilizatsii.

In the immobilized rats bemithyl (50 mg/kg in a single dose) was shown to normalize the state of the musculomotor and cardiovascular systems exerting the positive influence on the key links of the process of autoregulation in the form of the sedative (the central nervous system), stress-protective (hormonal regulation) and antihypoxic (metabolism) effects that characterizes it as the drug with the distinct antistress activity.

[Various biochemical survival mechanisms in highly-resistant animals]. / O nekotorykh biokhimicheskikh mekhanizmakh zhizneobespecheniia u vysoko-rezistentnykh zhivotnykh.

It was demonstrated in experiments on albino rats subjected to hypoxic hypoxia or hypothermia that highly-resistant animals, accounting for 30% of the population, survive much longer than animals with low and moderate resistance because extreme factors activate in them the system of peroxidase enzymes destroying the peroxides with the liberation of oxygen, which is then included in energy metabolism.

[Therapeutic efficacy of a new antihypoxic agent, ethomerzol, in experimental hemorrhagic shock]. / Lechebnaia éffektivnost' novogo antigipoksanta étomerzola pri éksperimental'nom gemorragicheskom shoke.

The antishock efficacy of a new antihypoxant ethomerzol was studied in cats with experimental hemorrhagic shock. Ethomerzol raised the therapeutic efficacy of infusion therapy with isotonic sodium chloride solution. It was found that the agent improves systemic hemodynamics and peripheral circulation. On grounds of analysis of the experimental data it is concluded that the inclusion of ethomerzol in the schedule of infusion therapy in hemorrhagic shock is expedient.

[Participation of dihydropyridine-sensitive calcium channels in psychotropic effects of nootropic drugs]. / Uchastie digidropiridinchuvstvitel'nykh Ca-kanalov v psikhotropnom éffekte nootropnykh preparatov.

Administration of Ca-entry blockers with different chemical structure before the braining sessions produced the reduction of memory retention in mice and rats in the one-trial passive avoidance tests. This effect was absent in animals treated immediately after training test. Nootropic drugs piracetam and oxiracetam corrected the retention of memory when injected just after training test. Chronic treatment of rats with increasing doses of the nootropic drugs produced about two-fold tissue-specific elevation in the density of DHP-receptors, associated with L-type Ca-channels in synaptosomal membranes of rat cerebral cortex. Maximal effect was observed in a dose of 10 mg/kg. Diltiazem, administrated in a dose of 10 mg/kg, produced about two-fold decrease in the receptors density measured 24 hrs after the first injection. Oxiracetam (10 mg/kg) completely antagonized the effect of Ca-entry blocker. These data imply that nootropic action of piracetam and oxiracetam is mediated by L-type Ca-channels.

[The effect of vestibuloprotectors on the cyclic nucleotide system in experimental motion sickness]. / Vliianie vestibuloprotektorov na sistemu tsiklicheskikh nukleotidov pri modelirovanii bolezni dvizheniia.

Changes in the blood plasma cyclic nucleotide (cAMP and cGMP) level under the effect of vestibuloprotectors: bemytil and etoxibemytil were studied in rats with experimental motion sickness. It is established that rotation causes increase in the cAMP level and decrease in the cGMP level. The effect of the vestibuloprotectors is determined by the dose of the drug and is aimed first of all at maintaining a stable cAMP level in vestibular exertion. Under conditions of this experiment etoxibemytil was more effective than bemytil.

[Characteristics of the anti-arrhythmia effect of phosphocreatine in the acute stage of experimental myocardial infarction]. / Osobennosti antiaritmicheskoi aktivnosti fosfokreatina v ostroi stadii éksperimental'nogo infarkta miokarda.

Antiarrhythmic and antifibrillatory effects of exogenous phosphocreatine, administered to animals at different dates after the onset of experimental myocardial infarction, were examined. Experiments were carried out on anesthetized dogs with acute one-step coronary artery ligation or in waking dogs 24 to 48 hours after two-step ligation of the descending branch of the left coronary artery (Harris's method). Major cardiac functional and hemodynamic parameters and ECG were recorded. The values obtained, using these models, show that exogenous phosphocreatine possesses high antiarrhythmic and antifibrillatory activities within first hours of coronary occlusion and is less effective after 24 hours of infarction.

[Effect of actoprotectors on the work capacity of operators during modeling of various factors of space flight]. / Vliianie aktoprotektorov na rabotosposobnost' operatorov v usloviiakh modelirovaniia nekotorykh faktorov kosmicheskogo poleta.

This paper presents experimental findings indicating that bemithyl, an actoprotective agent, has a beneficial effect on the health status and work capacity of operators during simulated space flight and 56-hour continuous work. The drug enhanced psychophysiological tolerance of the operators and improved the quality of their work: the quality of their compensatory tracking was on the average 10% higher, the number of errors of their porsuit tracking was 1.8 times lower, and the time of visual signal detection was 2.4 times shorter as compared to the placebo controls.

[Use of the new psychotropic preparation bemitil in treating asthenic disorders (clinico-pharmacological research)]. / Primenenie novogo psikhotropnogo preparata bemitila pri lechenii astenicheskikh narushenii (kliniko-farmakologicheskoe issledovanie).

In a series of 130 patients with asthenic conditions related to borderline forms of neuro-mental disturbances the authors compared clinico-pharmacological action of the actoprotector bemitil with that of nootropic drugs (piracetam and piridotol). The treatment with bemitil was either continuous or intermittent, being conducted according to the scheme elaborated in the course of the study. Bemitil proved to be more effective than piracetam and piriditol in relation to its influence on the manifestations of the asthenic symptom complex in general. Its application was characterized by a faster onset of the therapeutic effect and a peculiar mild psychostimulating action, primarily manifested in the impact on obligate manifestations of the asthenic disorders. The degree of the psychotropic action of the drug was found to be subject to changes depending on the scheme of its use.

[Structural analysis of the functional status of the brain as affected by bemethyl using pattern recognition theory]. / Analiz struktury funktsional'nogo sostoianiia mozga pri deistvii bemitila metodami teorii raspoznavaniia obrazov.

Evoked visual potentials in associated, parietal and second somatosensory zones of the neocortex were analysed in trained cats using implanted electrodes. The influence of bemethyl on the structure of behavioral reactions was analysed using theoretical methods of perceptual images, particularly the method of cluster analysis. Bemethyl was shown to increase the level of interaction between the functional elements of the system, leading to a more stable resolution of problems facing the system, as compared to the initial state.

[Participation of cholinergic systems in the recovery period following acute hypobaric hypoxia]. / Uchastie kholinergicheskikh sistem v periode vosstanovleniia posle ostroi gipobaricheskoi gipoksii.

The influence of some cholinergic drugs has been studied during prophylactic treatment and the recovery period after acute hypobaric hypoxia (AHBH) on AHBH model. Cholinolytics and cholinomimetics were shown to produce different effects on the animal resistance to AHBH, their role in the formation of resistance to hypoxia depending on the type of animal, the extent of hypoxic damage and duration of the recovery period after primary AHBH. The experiments performed suggest an important role of cholinergic system in the formation of hypoxic resistance in animals.

[Bemetil pharmacokinetics in an experiment on rats]. / Izuchenie farmakokinetiki bemitila v éksperiemnte u krys.

Pharmacokinetics of bemetil (2-ethyl-mercaptobenzimidazole), a representative of the group of actoprotectors, was studied at intravenous and intragastric administration during the experiment on rats by using gas-liquid chromatography. It was found that at intragastric administration the drug rapidly appeared in the systemic circulation, reached the maximal concentration in one hour; the character of bemetil elimination from the blood was biexponential at both routes of administration. The two-compartment model was used for calculation of the main pharmacokinetic constants and bioavailability. The analysis of the experimental findings on urinary excretion of bemetil made it possible to conclude that little amount of the drug (0.56%) is excreted in the urine in the unchanged form; most amount of bemetil is excreted in the form of metabolites and in the bound state.

[Antihypoxic activity of cytochrome c heme peptides]. / Antigpoksicheskaia aktivnost' gem-peptidov tsitokhroma c.

A comparative study of antihypoxic activity of five and two cytochrome c derivatives was performed during their single prophylactic administration on the model of acute hypobaric hypoxia (AHBH) and during rehabilitation period after AHBH, respectively. Antihypoxic efficiency of cytochrome c derivatives was shown to be dependent on doses, time of drug administration, and type of experimental animal resistance. The heme-nonapeptide of cytochrome c proved to be of maximum efficiency during prophylactic administration and rehabilitation period after AHBH.

[Experimental study of the antihypoxic properties of ibuprofen and other nonsteroidal anti-inflammatory preparations]. / Eksperimental'noe izuchenie antigipoksicheskikh svoistv ibuprofena i drugikh nesteroidnykh protivovospalitel'nykh preparatov.

The antihypoxic properties of ibuprofen, diclofenac sodium, acetylsalicylic acid and phenylbutazone have been studied. Ibuprofen significantly increases survival of mice in the model of hypoxic hypoxia with hypercapnia. In addition, ibuprofen and diclofenac sodium possess antihypoxic protective activity in the models of circulatory and anoxic hypoxia in rats.

[Experimental and clinical data on the ability of bemetil to penetrate the hemato-encephalic barrier]. / Eksperimental'nye i klinicheskie dannye o sposobnosti bemetila pronikat' cherez gematoéntsefalicheskii bar'er.

Experimental and clinical data indicated bemetil ability to penetrate through the blood-brain barrier. Bemetil concentration in the rat brain tissue was found to be significantly higher than in the plasma. Its concentration in the cerebrospinal fluid of patients with craniocerebral trauma was lower than in the plasma; the latter however does not exclude the possibility of bemetil accumulation in the brain structures.

[Pharmacokinetics and the clinical effect of bemitil after a single administration]. / Farmakokinetika i klinicheskii éffekt bemitila posle odnokratnogo primeneniia.

It was found on studying a novel psychotropic drug bemitil that after its single administration kinetic curves significantly differed depending on a clinical effect of the test dose in patients with asthenic states. At predomination of the psychoactivating component of action one could note a larger area under the concentration-time relationship curve and a shorter period of half-excretion than in patients with the tranquilizing action. The obtained data on the difference in the drug test dose effect depending on the drug pharmacokinetics should be taken into consideration at determination of bemitil course therapy duration in patients with neuroses and neurosis-like states with predominance of asthenic disturbances in the clinical picture.