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1.
Eksp Klin Farmakol ; 73(7): 13-5, 2010 Jul.
Artigo em Russo | MEDLINE | ID: mdl-20821973

RESUMO

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.


Assuntos
Córtex Cerebral/efeitos dos fármacos , Imobilização , Nootrópicos/farmacologia , Piracetam/farmacologia , Receptores de GABA-A/metabolismo , Ácido gama-Aminobutírico/análogos & derivados , Animais , Córtex Cerebral/metabolismo , Masculino , Ratos , Fatores de Tempo , Ácido gama-Aminobutírico/farmacologia
2.
Biomed Khim ; 53(3): 307-12, 2007.
Artigo em Russo | MEDLINE | ID: mdl-17722581

RESUMO

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.


Assuntos
Aminoácidos/análise , Metabolismo Energético , Fígado/química , Movimento , Miocárdio/química , Animais , Cromatografia Líquida de Alta Pressão , Ratos , Restrição Física
3.
Eksp Klin Farmakol ; 69(2): 3-5, 2006.
Artigo em Russo | MEDLINE | ID: mdl-16845930

RESUMO

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.


Assuntos
Ansiolíticos/uso terapêutico , Ansiedade/prevenção & controle , Benzimidazóis/uso terapêutico , Isquemia Encefálica/complicações , Agonistas GABAérgicos/uso terapêutico , Morfolinas/uso terapêutico , Animais , Ansiolíticos/administração & dosagem , Ansiedade/etiologia , Benzimidazóis/administração & dosagem , Agonistas GABAérgicos/administração & dosagem , Infarto da Artéria Cerebral Média/fisiopatologia , Aprendizagem em Labirinto/efeitos dos fármacos , Morfolinas/administração & dosagem , Ratos , Ratos Endogâmicos
4.
Eksp Klin Farmakol ; 69(2): 10-3, 2006.
Artigo em Russo | MEDLINE | ID: mdl-16845932

RESUMO

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.


Assuntos
Depressão/tratamento farmacológico , Hipocinesia/complicações , Nootrópicos/uso terapêutico , Piracetam/uso terapêutico , Receptores de GABA-A/deficiência , Ácido gama-Aminobutírico/análogos & derivados , Animais , Encéfalo/metabolismo , Depressão/etiologia , Depressão/metabolismo , Hipocinesia/metabolismo , Masculino , Ratos , Ratos Endogâmicos , Ácido gama-Aminobutírico/uso terapêutico
5.
Eksp Klin Farmakol ; 68(5): 36-9, 2005.
Artigo em Russo | MEDLINE | ID: mdl-16277209

RESUMO

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.


Assuntos
Colchicina/farmacologia , Febre Familiar do Mediterrâneo/imunologia , Granulócitos/efeitos dos fármacos , Iodo/uso terapêutico , Lítio/uso terapêutico , Monócitos/efeitos dos fármacos , Fagocitose/efeitos dos fármacos , Adolescente , Adulto , Dextrinas , Portadores de Fármacos , Feminino , Granulócitos/imunologia , Humanos , Masculino , Monócitos/imunologia
6.
Eksp Klin Farmakol ; 68(6): 36-9, 2005.
Artigo em Russo | MEDLINE | ID: mdl-16405032

RESUMO

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.


Assuntos
Colchicina/farmacologia , Febre Familiar do Mediterrâneo/metabolismo , Supressores da Gota/farmacologia , Granulócitos/metabolismo , Monócitos/metabolismo , Explosão Respiratória/efeitos dos fármacos , Adolescente , Adulto , Células Cultivadas , Quimiotaxia/efeitos dos fármacos , Febre Familiar do Mediterrâneo/patologia , Feminino , Humanos , Ativação de Macrófagos/efeitos dos fármacos , Masculino , Ativação de Neutrófilo/efeitos dos fármacos , Fagocitose/efeitos dos fármacos , Proteína Quinase C/metabolismo
7.
Eksp Klin Farmakol ; 66(5): 6-9, 2003.
Artigo em Russo | MEDLINE | ID: mdl-14650205

RESUMO

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).


Assuntos
Córtex Cerebral/metabolismo , Hipocinesia/metabolismo , Lipídeos de Membrana/metabolismo , Sinaptossomos/metabolismo , Ácido gama-Aminobutírico/farmacologia , Animais , Ácido Araquidônico/metabolismo , Córtex Cerebral/citologia , Córtex Cerebral/efeitos dos fármacos , Fosfatidilinositóis/metabolismo , Ratos , Receptores de GABA-B/metabolismo , Sinaptossomos/efeitos dos fármacos
8.
Mikrobiologiia ; 72(4): 493-7, 2003.
Artigo em Russo | MEDLINE | ID: mdl-14526539

RESUMO

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.


Assuntos
Bactérias Aeróbias Gram-Negativas/metabolismo , Ferro/metabolismo , Sulfetos/metabolismo , Acidithiobacillus/metabolismo , Compostos Ferrosos/metabolismo , Bactérias Aeróbias Gram-Negativas/crescimento & desenvolvimento , Concentração de Íons de Hidrogênio , Oxirredução , Microbiologia do Solo , Bactérias Redutoras de Enxofre , Temperatura
9.
Eksp Klin Farmakol ; 66(3): 4-8, 2003.
Artigo em Russo | MEDLINE | ID: mdl-12924223

RESUMO

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.


Assuntos
Adaptação Fisiológica , Circulação Cerebrovascular , Hipocinesia/metabolismo , Hipocinesia/fisiopatologia , Ácido gama-Aminobutírico/fisiologia , Animais , Humanos
10.
Vopr Med Khim ; 48(5): 485-9, 2002.
Artigo em Russo | MEDLINE | ID: mdl-12498091

RESUMO

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.


Assuntos
Difosfato de Adenosina/metabolismo , Hipocinesia/metabolismo , Mitocôndrias Hepáticas/metabolismo , Nootrópicos/farmacologia , Piracetam/farmacologia , Ácido gama-Aminobutírico/farmacologia , Animais , Masculino , Mitocôndrias Hepáticas/efeitos dos fármacos , Mitocôndrias Hepáticas/enzimologia , Fosforilação , Ratos , Succinato Desidrogenase/metabolismo
11.
Eksp Klin Farmakol ; 63(5): 41-3, 2000.
Artigo em Russo | MEDLINE | ID: mdl-11109525

RESUMO

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.


Assuntos
Vasos Sanguíneos/patologia , Hipocinesia/sangue , Piracetam/farmacologia , Inibidores da Agregação Plaquetária/farmacologia , Ácido gama-Aminobutírico/farmacologia , Animais , Hipocinesia/patologia , Hipocinesia/fisiopatologia , Masculino , Atividade Motora , Agregação Plaquetária/efeitos dos fármacos , Ratos
12.
Eksp Klin Farmakol ; 61(5): 15-7, 1998.
Artigo em Russo | MEDLINE | ID: mdl-9854625

RESUMO

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.


Assuntos
Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Bloqueadores dos Canais de Cálcio/farmacologia , Cinarizina/farmacologia , Flunarizina/farmacologia , Hipocinesia/metabolismo , Ácido gama-Aminobutírico/efeitos dos fármacos , Ácido gama-Aminobutírico/metabolismo , Animais , Química Encefálica/efeitos dos fármacos , Radioisótopos de Carbono , Circulação Cerebrovascular/efeitos dos fármacos , Hipocinesia/fisiopatologia , Masculino , Ratos , Restrição Física , Fatores de Tempo , Ácido gama-Aminobutírico/farmacologia
13.
Eksp Klin Farmakol ; 61(5): 62-4, 1998.
Artigo em Russo | MEDLINE | ID: mdl-9854639

RESUMO

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.


Assuntos
GABAérgicos/uso terapêutico , Hipocinesia/tratamento farmacológico , Equilíbrio Hidroeletrolítico/efeitos dos fármacos , Animais , Avaliação Pré-Clínica de Medicamentos , Eletrólitos/sangue , Hipocinesia/sangue , Masculino , Piracetam/uso terapêutico , Ratos , Fatores de Tempo , Ácido gama-Aminobutírico/uso terapêutico
14.
Vopr Med Khim ; 44(3): 262-6, 1998.
Artigo em Russo | MEDLINE | ID: mdl-9703626

RESUMO

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.


Assuntos
Adenosina Trifosfatases/metabolismo , Encéfalo/efeitos dos fármacos , Hipocinesia/enzimologia , Mitocôndrias Hepáticas/efeitos dos fármacos , Piracetam/farmacologia , Ácido gama-Aminobutírico/farmacologia , 2,4-Dinitrofenol/farmacologia , Animais , Encéfalo/metabolismo , Ativação Enzimática , Magnésio/metabolismo , Masculino , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Mitocôndrias Hepáticas/metabolismo , Ratos
15.
Eksp Klin Farmakol ; 60(5): 31-4, 1997.
Artigo em Russo | MEDLINE | ID: mdl-9483402

RESUMO

Experiments on rats showed that the morpho-functional state of the cerebral cortex microcirculatory bed suffers marked changes in different periods of hypokinesia. This was accompanied with obvious morphological changes in the brain, the development of brain edema in particular. It was found that the GABAergic agents which we used ranked below Ca-antagonists in antiedemic activity.


Assuntos
Encéfalo/efeitos dos fármacos , Bloqueadores dos Canais de Cálcio/farmacologia , Circulação Cerebrovascular/efeitos dos fármacos , GABAérgicos/farmacologia , Animais , Bicuculina/farmacologia , Encéfalo/patologia , Encéfalo/fisiopatologia , Edema Encefálico/prevenção & controle , Dioxanos/farmacologia , Feminino , Antagonistas GABAérgicos/farmacologia , Antagonistas de Receptores de GABA-A , Masculino , Microcirculação/efeitos dos fármacos , Nifedipino/farmacologia , Piracetam/farmacologia , Ratos , Ratos Wistar , Restrição Física , Tiazóis/farmacologia , Verapamil/farmacologia , Ácido gama-Aminobutírico/farmacologia
16.
Eksp Klin Farmakol ; 59(3): 40-3, 1996.
Artigo em Russo | MEDLINE | ID: mdl-8974583

RESUMO

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.


Assuntos
Encéfalo/efeitos dos fármacos , Hipocinesia/tratamento farmacológico , Fármacos Neuroprotetores/uso terapêutico , Fosfolipídeos/metabolismo , Piracetam/uso terapêutico , Ácido gama-Aminobutírico/uso terapêutico , Animais , Encéfalo/metabolismo , Química Encefálica/efeitos dos fármacos , Cromatografia em Camada Fina , Avaliação Pré-Clínica de Medicamentos , Hipocinesia/metabolismo , Masculino , Fosfolipídeos/análise , Ratos , Fatores de Tempo
17.
Eksp Klin Farmakol ; 58(5): 16-8, 1995.
Artigo em Russo | MEDLINE | ID: mdl-8704580

RESUMO

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.


Assuntos
Circulação Cerebrovascular/efeitos dos fármacos , Hipocinesia/sangue , Hipocinesia/fisiopatologia , Inibidores da Agregação Plaquetária/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Adaptação Fisiológica/efeitos dos fármacos , Adulto , Animais , Repouso em Cama , Encéfalo/irrigação sanguínea , Humanos , Masculino , Microcirculação/efeitos dos fármacos , Microcirculação/fisiopatologia , Pessoa de Meia-Idade , Inibidores da Agregação Plaquetária/uso terapêutico , Ratos , Valores de Referência , Fatores de Tempo
18.
Eksp Klin Farmakol ; 58(4): 23-5, 1995.
Artigo em Russo | MEDLINE | ID: mdl-7580746

RESUMO

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.


Assuntos
Circulação Cerebrovascular/fisiologia , Hipercapnia/fisiopatologia , Hipocinesia/fisiopatologia , Hipotensão/fisiopatologia , Sistema Vasomotor/fisiologia , Ácido gama-Aminobutírico/farmacologia , Animais , Circulação Cerebrovascular/efeitos dos fármacos , Estimulação Elétrica , Nervo Femoral , Hipotensão/induzido quimicamente , Coelhos , Ratos , Restrição Física , Fatores de Tempo , Trimetafano , Vasodilatadores , Sistema Vasomotor/efeitos dos fármacos
19.
Eksp Klin Farmakol ; 57(5): 16-7, 1994.
Artigo em Russo | MEDLINE | ID: mdl-7696894

RESUMO

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.


Assuntos
4-Butirolactona/farmacologia , Circulação Cerebrovascular/efeitos dos fármacos , Malondialdeído/antagonistas & inibidores , Pirrolidinonas/farmacologia , Vasoconstrição/efeitos dos fármacos , Ácido gama-Aminobutírico/farmacologia , Animais , Antioxidantes/farmacologia , Gatos , Interações Medicamentosas , Malondialdeído/farmacologia
20.
Eksp Klin Farmakol ; 56(5): 8-11, 1993.
Artigo em Russo | MEDLINE | ID: mdl-8312821

RESUMO

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.


Assuntos
Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Imobilização/fisiologia , Animais , Bicuculina/farmacologia , Encéfalo/patologia , Dióxido de Carbono/metabolismo , Radioisótopos de Carbono , Masculino , Reação do Ácido Periódico de Schiff , Ratos , Fatores de Tempo , Ácido gama-Aminobutírico/farmacologia
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