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1.
Eksp Klin Farmakol ; 73(7): 13-5, 2010 Jul.
Article in Russian | MEDLINE | ID: mdl-20821973

ABSTRACT

The influence of picamilon and piracetam on the quantitative changes in the central GABA(A) macromolecular receptor complexes in the rat brain has been investigated under the experimental conditions of hypokinesia. It was found that the injection of these nootropes under the conditions of 7-day hypokinesia and 4-day recovery period did not show visible changes in the amount of active GABA(A) receptors. However, the injection of picamilon under the conditions of 15-day hypokinesia and 8-day recovery period showed a tendency to restoration of the number of active GABA(A) receptors.


Subject(s)
Cerebral Cortex/drug effects , Immobilization , Nootropic Agents/pharmacology , Piracetam/pharmacology , Receptors, GABA-A/metabolism , gamma-Aminobutyric Acid/analogs & derivatives , Animals , Cerebral Cortex/metabolism , Male , Rats , Time Factors , gamma-Aminobutyric Acid/pharmacology
2.
Biomed Khim ; 53(3): 307-12, 2007.
Article in Russian | MEDLINE | ID: mdl-17722581

ABSTRACT

The contents of the free amino acid in the liver and heart tissues were investigated under conditions of experimental hypokinesia on 15th, 30th and 45th days by means of HPLC method. The content of glutamate and aspartate in the liver tissue was sharply decreased with the increase of the hypokinesia period. The degree of the decrease of aspartate was more pronounced than glutamate. The level of glycine in the liver remained unchanged on 15th and 45th days of hypokinesia but increased on the 30th day compared with control animals. There were insignificant changes in taurine content. In contrast to the liver tissue the contents of monoaminodicarbonic acids were increased in the myocardum. The content of taurine was decreased over the whole period of restricted movement activity compared with control, especially on the 15th day of hypokinesia. The changes of free amino acids are discussed in terms of their participation in energy metabolism of both tissues during the restricted movement activity.


Subject(s)
Amino Acids/analysis , Energy Metabolism , Liver/chemistry , Movement , Myocardium/chemistry , Animals , Chromatography, High Pressure Liquid , Rats , Restraint, Physical
3.
Eksp Klin Farmakol ; 69(2): 3-5, 2006.
Article in Russian | MEDLINE | ID: mdl-16845930

ABSTRACT

The ability of afobazole, a selective anxiolytic to prevent the brain local ischemia-induced anxiety has been studied in experiments on rats. It is established that middle cerebral artery occlusion (MCAO) is accompanied by the development of anxiety, the degree of which increases with the duration of occlusion. Afobazole in a doze of 1 mg/kg administrated during 6 days after MCAO prevents the development of anxiety. The effect is manifested by positive changes in the parameters describing the behavior of animals in elevated plus maze test. No tolerance to the drug is developed during continuous afobazole injection within 12 days after MCAO. The experimental data indicate that the well-known anxiolytic action of afobazole is also well pronounced under the conditions of a local cerebrtal ischemia.


Subject(s)
Anti-Anxiety Agents/therapeutic use , Anxiety/prevention & control , Benzimidazoles/therapeutic use , Brain Ischemia/complications , GABA Agonists/therapeutic use , Morpholines/therapeutic use , Animals , Anti-Anxiety Agents/administration & dosage , Anxiety/etiology , Benzimidazoles/administration & dosage , GABA Agonists/administration & dosage , Infarction, Middle Cerebral Artery/physiopathology , Maze Learning/drug effects , Morpholines/administration & dosage , Rats , Rats, Inbred Strains
4.
Eksp Klin Farmakol ; 69(2): 10-3, 2006.
Article in Russian | MEDLINE | ID: mdl-16845932

ABSTRACT

The influence of a 15-day hypokinesia on the development of anxiety-depression state and quantitative changes in the central GABA-A macromolecular receptor complexes in the rat brain has been investigated under conditions of the despair (forced swim) test. Simultaneously, the effects of well-known nootropic drugs picamilon and piracetam on the dynamics of state parameters in the experimental animals have been evaluated. It was found that hypokinesia led to the development of anxiety and depression accompanied by reduction in the amount of active GABA-A receptors. The injections of piracetam and picamilon showed a tendency to restoration of the number of active GABA-A receptors and to normalization of the behavioral parameters.


Subject(s)
Depression/drug therapy , Hypokinesia/complications , Nootropic Agents/therapeutic use , Piracetam/therapeutic use , Receptors, GABA-A/deficiency , gamma-Aminobutyric Acid/analogs & derivatives , Animals , Brain/metabolism , Depression/etiology , Depression/metabolism , Hypokinesia/metabolism , Male , Rats , Rats, Inbred Strains , gamma-Aminobutyric Acid/therapeutic use
5.
Eksp Klin Farmakol ; 68(5): 36-9, 2005.
Article in Russian | MEDLINE | ID: mdl-16277209

ABSTRACT

Disturbances in the regulation of phagocytic activity of neutrophils and monocytes (PANM) in whole peripheral blood of patients with familial Mediterranean Fever (FMF), which had not received treatment with colchicines, were determined by quantitative flow cytofluorimetry. The effect of iodine-lithium-alpha-dextrin (armenicum) and colchicine on the PANM in the blood of FMF patients was studied in vitro. The intensity of phagocytosis in populations of neutrophils and monocytes in FMF patients (n = 6) during the remission period is higher than that during the FMF attack (n = 6) and higher than in healthy donors (n = 9). The PANM in patients during the FMF attack is higher compared to that in healthy donors. Iodine-lithium-alpha-dextrin (armenicum) and colchicine inhibited the phagocytosis of effector cells in FMF patients in a dose-dependent and time-dependent manner. It was shown that the suppressive effect of the drugs increased with decreasing bacteria/effector cells ratio.


Subject(s)
Colchicine/pharmacology , Familial Mediterranean Fever/immunology , Granulocytes/drug effects , Iodine/therapeutic use , Lithium/therapeutic use , Monocytes/drug effects , Phagocytosis/drug effects , Adolescent , Adult , Dextrins , Drug Carriers , Female , Granulocytes/immunology , Humans , Male , Monocytes/immunology
6.
Eksp Klin Farmakol ; 68(6): 36-9, 2005.
Article in Russian | MEDLINE | ID: mdl-16405032

ABSTRACT

The influence of colchicine on the spontaneous and chemotaxis-, protein kinase C-, and phagocytosis-induced respiratory burst of neutrophils and monocytes in the peripheral blood of patients with familial Mediterranean fever (FMF) has been studied. The transient activation of neutrophils and monocytes on the level of a single cell has been monitored by means of flow cytofluorimetry. It is shown that colchicine blocks the induction of chemotaxis-, phagocytosis-, and proteinkinase C-dependent respiratory burst in vitro, as well as the increased pro-oxidant transient activation of neutrophils and monocytes of FMF patients, both in the period of remission and during the FMF attack. Colchicine stimulates the intensity of the spontaneous respiratory burst of neutrophils and monocytes in patients in the course of remission and during the FMF attack. At the same time, the drug effectively suppresses the periodicity of the multidirectional transient activation of the respiratory burst of effector cells during FMF.


Subject(s)
Colchicine/pharmacology , Familial Mediterranean Fever/metabolism , Gout Suppressants/pharmacology , Granulocytes/metabolism , Monocytes/metabolism , Respiratory Burst/drug effects , Adolescent , Adult , Cells, Cultured , Chemotaxis/drug effects , Familial Mediterranean Fever/pathology , Female , Humans , Macrophage Activation/drug effects , Male , Neutrophil Activation/drug effects , Phagocytosis/drug effects , Protein Kinase C/metabolism
7.
Eksp Klin Farmakol ; 66(5): 6-9, 2003.
Article in Russian | MEDLINE | ID: mdl-14650205

ABSTRACT

The influence of a 30-day hypokinesia on the phosphoinositide cycle (PIC) initiation and on the inclusion of [14C]-arachidonic acid into cerebral synaptosome phospholipids was studied in rats. The results show that the catabolism of phospholipids prevails on the background of signal transduction in synaptosomes on the 30th day of hypokinesia. The effect of gamma-aminobutyric acid (GABA) is manifested by a sharp increase in the PIC activity 5 sec upon initiation and leads to normalization of the PIC activity in the late stage (5 min).


Subject(s)
Cerebral Cortex/metabolism , Hypokinesia/metabolism , Membrane Lipids/metabolism , Synaptosomes/metabolism , gamma-Aminobutyric Acid/pharmacology , Animals , Arachidonic Acid/metabolism , Cerebral Cortex/cytology , Cerebral Cortex/drug effects , Phosphatidylinositols/metabolism , Rats , Receptors, GABA-B/metabolism , Synaptosomes/drug effects
8.
Mikrobiologiia ; 72(4): 493-7, 2003.
Article in Russian | MEDLINE | ID: mdl-14526539

ABSTRACT

Two strains of Leptospirillum-like bacteria isolated from dumps of Alaverdi and Akhtala sulfide ore deposits in Armenia were studied. The optimum and maximum temperatures for the growth of both strains were 37 and 40 degrees C, respectively. The pH optimum was 2.0-2.3. Bacterial growth and ferrous iron oxidation were inhibited by yeast extract. The pyrite-leaching activity of the Leptospirillum-like bacteria under mesophilic conditions was close to that of Acidithiobacillus ferroxidans and exceeded by 2.0-2.7 times the activity of these moderately thermophilic bacteria at 37 degrees C. The leaching of pyrite by Leptospirillum-like bacteria increased in the presence of sulfur-oxidizing bacteria, particularly, in their association with a thermotolerant sulfur-oxidizing bacterium.


Subject(s)
Gram-Negative Aerobic Bacteria/metabolism , Iron/metabolism , Sulfides/metabolism , Acidithiobacillus/metabolism , Ferrous Compounds/metabolism , Gram-Negative Aerobic Bacteria/growth & development , Hydrogen-Ion Concentration , Oxidation-Reduction , Soil Microbiology , Sulfur-Reducing Bacteria , Temperature
9.
Eksp Klin Farmakol ; 66(3): 4-8, 2003.
Article in Russian | MEDLINE | ID: mdl-12924223

ABSTRACT

Hypokinesia involves a number of significant biochemical, histochemical, and pathophysiological changes in brain tissues, vessels, and neurocytes, including glucose metabolism disturbances, calcium level violation and transduction in synaptosomes, changes, on the levels of neuroactive amino acids, nitric oxide, and lipid peroxidation products. All these variations depend on the terms of hypokinesia. It is established that GABA, together with other neuromediators, play an important role in the adaptation process. GABAergic drugs produce effects indicative of the activation of processes leading to compensation and, probably, elimination of the aforementioned negative changes.


Subject(s)
Adaptation, Physiological , Cerebrovascular Circulation , Hypokinesia/metabolism , Hypokinesia/physiopathology , gamma-Aminobutyric Acid/physiology , Animals , Humans
10.
Vopr Med Khim ; 48(5): 485-9, 2002.
Article in Russian | MEDLINE | ID: mdl-12498091

ABSTRACT

Long-term limitation of motor activity of male rats is accompanied by impairments of mitochondrial ADP phosphorylation in liver and heart. The most significant changes were observed after 15 and 45 days of hypokinesia. Administration of GABA and pyracetam to animals subjected to hypokinesia induced a tendency to "normalization" of ADP phosphorilation processes.


Subject(s)
Adenosine Diphosphate/metabolism , Hypokinesia/metabolism , Mitochondria, Liver/metabolism , Nootropic Agents/pharmacology , Piracetam/pharmacology , gamma-Aminobutyric Acid/pharmacology , Animals , Male , Mitochondria, Liver/drug effects , Mitochondria, Liver/enzymology , Phosphorylation , Rats , Succinate Dehydrogenase/metabolism
11.
Eksp Klin Farmakol ; 63(5): 41-3, 2000.
Article in Russian | MEDLINE | ID: mdl-11109525

ABSTRACT

Restricted motor activity on the background of platelet hyperaggregation in the whole blood and plasma leads to inhibition of the antiaggregant activity of the blood vessel wall, thus creating prerequisites for the development of thromboembolic disturbances. Under these conditions, GABA and piracetam produce a pronounced protective action with respect to the platelet-vessel wall interactions.


Subject(s)
Blood Vessels/pathology , Hypokinesia/blood , Piracetam/pharmacology , Platelet Aggregation Inhibitors/pharmacology , gamma-Aminobutyric Acid/pharmacology , Animals , Hypokinesia/pathology , Hypokinesia/physiopathology , Male , Motor Activity , Platelet Aggregation/drug effects , Rats
12.
Eksp Klin Farmakol ; 61(5): 15-7, 1998.
Article in Russian | MEDLINE | ID: mdl-9854625

ABSTRACT

Studies showed that 15-day restriction of motor activity inhibits the reuptake of GABA by sections of the rat brain cortex and hypothalamus. In prolonged intraperitoneal injection of 10 mg/kg cinnarizine in hyperkinesia, further inhibition of this process in hypothalamic sections is encountered on the 15th days. Flunarizin (1 mg/kg) administered in a like manner has no significant effect on GABA reuptake. A course of GABA injections in a dose of 5 mg/kg improves in rats with restricted motor activity the local blood flow in the frontal lobe of the brain.


Subject(s)
Brain/drug effects , Brain/metabolism , Calcium Channel Blockers/pharmacology , Cinnarizine/pharmacology , Flunarizine/pharmacology , Hypokinesia/metabolism , gamma-Aminobutyric Acid/drug effects , gamma-Aminobutyric Acid/metabolism , Animals , Brain Chemistry/drug effects , Carbon Radioisotopes , Cerebrovascular Circulation/drug effects , Hypokinesia/physiopathology , Male , Rats , Restraint, Physical , Time Factors , gamma-Aminobutyric Acid/pharmacology
13.
Eksp Klin Farmakol ; 61(5): 62-4, 1998.
Article in Russian | MEDLINE | ID: mdl-9854639

ABSTRACT

The effect of hypokinesia on the blood electrolyte balance was studied. In restricted motor activity marked deviations of the type of hypokalemia and hypercalcemia were encountered, which could promote the development of various pathological processes, including disorder of central and regional hemodynamics. GABA and piracetam had no effect on the blood serum electrolyte content in the early periods of hypokinesia. In later periods of hypokinesia both drugs under examination corrected the disorders of blood electrolyte balance induced by prolonged restriction of motor activity.


Subject(s)
GABA Agents/therapeutic use , Hypokinesia/drug therapy , Water-Electrolyte Balance/drug effects , Animals , Drug Evaluation, Preclinical , Electrolytes/blood , Hypokinesia/blood , Male , Piracetam/therapeutic use , Rats , Time Factors , gamma-Aminobutyric Acid/therapeutic use
14.
Vopr Med Khim ; 44(3): 262-6, 1998.
Article in Russian | MEDLINE | ID: mdl-9703626

ABSTRACT

Long-term hypokinesia is accompanied by changes in the activity of Mg(2+) and 2,4-dinitrophenol (DNP)-stimulated ATPases of rat brain and liver mitochondria. These changes are phasic and especially pronounced at periods characterised by most pronounced metabolic alterations Treatment of animals with GABA and piracetam tends to normalise the enzyme activities.


Subject(s)
Adenosine Triphosphatases/metabolism , Brain/drug effects , Hypokinesia/enzymology , Mitochondria, Liver/drug effects , Piracetam/pharmacology , gamma-Aminobutyric Acid/pharmacology , 2,4-Dinitrophenol/pharmacology , Animals , Brain/metabolism , Enzyme Activation , Magnesium/metabolism , Male , Mitochondria/drug effects , Mitochondria/metabolism , Mitochondria, Liver/metabolism , Rats
16.
Eksp Klin Farmakol ; 59(3): 40-3, 1996.
Article in Russian | MEDLINE | ID: mdl-8974583

ABSTRACT

The influence of hypokinesia on phospholipid composition of the brain tissue was investigated. Hypokinesia was found to cause significant disorders in the phospholipid composition. Changes exhibit a phase character and are more pronounced on the 15-th and 30-th days of hypokinesia. The use of GABA and pyracetam promotes the processes aimed at normalization of the phospholipid metabolism in the brain tissue.


Subject(s)
Brain/drug effects , Hypokinesia/drug therapy , Neuroprotective Agents/therapeutic use , Phospholipids/metabolism , Piracetam/therapeutic use , gamma-Aminobutyric Acid/therapeutic use , Animals , Brain/metabolism , Brain Chemistry/drug effects , Chromatography, Thin Layer , Drug Evaluation, Preclinical , Hypokinesia/metabolism , Male , Phospholipids/analysis , Rats , Time Factors
17.
Eksp Klin Farmakol ; 58(5): 16-8, 1995.
Article in Russian | MEDLINE | ID: mdl-8704580

ABSTRACT

Changes in local cerebral blood flow and in microcirculatory channels in the cortex of rat brain were studied in conditions of early and remote hypokinesia. The rheological parameters of blood were studied in patients which stayed in ber for a long time in traumatological hospitals. We showed that by the 60th day of hypokinesia and in conditions of active readaptation the disordered cerebral blood flow starts to stabilize and tendency to normalization of some parameters of the cerebral blood flow and microcirculatory channels become clearly seen. The study of the functional state of the platelets showed that prescription of antiaggregants along with physical training can prevent thromboembolic aggravations associated with hypokinesia.


Subject(s)
Cerebrovascular Circulation/drug effects , Hypokinesia/blood , Hypokinesia/physiopathology , Platelet Aggregation Inhibitors/pharmacology , Platelet Aggregation/drug effects , Adaptation, Physiological/drug effects , Adult , Animals , Bed Rest , Brain/blood supply , Humans , Male , Microcirculation/drug effects , Microcirculation/physiopathology , Middle Aged , Platelet Aggregation Inhibitors/therapeutic use , Rats , Reference Values , Time Factors
18.
Eksp Klin Farmakol ; 58(4): 23-5, 1995.
Article in Russian | MEDLINE | ID: mdl-7580746

ABSTRACT

We studied the formation of vasomotor reflexes in hypokinesia and responses of the brain vessels to the action of GABA, hypotension, and hypercapnia. We found that the response of the brain vessels to GABA is delayed and the mechanisms which supported an adequate cerebral vasculation are distorted in hypotension. At the same time the disturbance of the reflectory reaction of the brain vessels in the course of forming the vasomotor reflexes and the absence of significant changes in response to GABA were noticed. The capability of GABA of inhibiting cerebral blood circulation arising in hypokinesia is shown.


Subject(s)
Cerebrovascular Circulation/physiology , Hypercapnia/physiopathology , Hypokinesia/physiopathology , Hypotension/physiopathology , Vasomotor System/physiology , gamma-Aminobutyric Acid/pharmacology , Animals , Cerebrovascular Circulation/drug effects , Electric Stimulation , Femoral Nerve , Hypotension/chemically induced , Rabbits , Rats , Restraint, Physical , Time Factors , Trimethaphan , Vasodilator Agents , Vasomotor System/drug effects
19.
Eksp Klin Farmakol ; 57(5): 16-7, 1994.
Article in Russian | MEDLINE | ID: mdl-7696894

ABSTRACT

GABA and its cyclic derivatives, gamma-butyrolactone and pyrrolidone-2, have been ascertained to abolish and prevent the cerebral vasoconstrictor effects of malonic dialdehyde. In this respect, gamma-butyrolactone excels pyrrolidone-2 and GABA, the effects of GABA being most slight. It may be suggested that the neuroactive amino acids exhibit antioxidative effects.


Subject(s)
4-Butyrolactone/pharmacology , Cerebrovascular Circulation/drug effects , Malondialdehyde/antagonists & inhibitors , Pyrrolidinones/pharmacology , Vasoconstriction/drug effects , gamma-Aminobutyric Acid/pharmacology , Animals , Antioxidants/pharmacology , Cats , Drug Interactions , Malondialdehyde/pharmacology
20.
Eksp Klin Farmakol ; 56(5): 8-11, 1993.
Article in Russian | MEDLINE | ID: mdl-8312821

ABSTRACT

Experiments on rats have established that hypokinetic life leads to morphological and metabolic changes in tissue. Simultaneously, there is a negative dynamics in rheological and vascular changes. GABAergic substances have been found to have a tendency to level off morphological changes from 15 to 45 days of experimental investigations, but no later and they are of great energy value for brain tissue by stimulation of glucose utilization rates.


Subject(s)
Brain/drug effects , Brain/metabolism , Immobilization/physiology , Animals , Bicuculline/pharmacology , Brain/pathology , Carbon Dioxide/metabolism , Carbon Radioisotopes , Male , Periodic Acid-Schiff Reaction , Rats , Time Factors , gamma-Aminobutyric Acid/pharmacology
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