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1.
Biull Eksp Biol Med ; 110(11): 503-4, 1990 Nov.
Artigo em Russo | MEDLINE | ID: mdl-1964606

RESUMO

Experiments on isolated strips of the rabbit uterus showed the stimulating effects of small doses of GABA, AOAA and phenibut on uterine contractility, while large doses exerted the reverse (suppressing) effects. Administration of bicuculline and picrotoxin before or after the above-mentioned drugs reduced their suppressing effects on uterine muscle contractility. The data postulate the involvement of GABAA and GABAB receptors in the drugs action on the rabbit uterus.


Assuntos
Ácido Amino-Oxiacético/farmacologia , Receptores de GABA-A/efeitos dos fármacos , Contração Uterina/efeitos dos fármacos , Ácido gama-Aminobutírico/análogos & derivados , Ácido gama-Aminobutírico/farmacologia , Animais , Bicuculina/farmacologia , Relação Dose-Resposta a Droga , Interações Medicamentosas , Feminino , Técnicas In Vitro , Picrotoxina/farmacologia , Coelhos , Receptores de GABA-A/fisiologia , Contração Uterina/fisiologia
2.
Farmakol Toksikol ; 53(5): 45-7, 1990.
Artigo em Russo | MEDLINE | ID: mdl-2253749

RESUMO

Phenibut and phentolamine were found to exhibit the properties of the true antioxidants in the hen egg yolk suspension and in the rat brain homogenate. The antioxidative activities of the drugs were significantly higher in the brain homogenate, while the antioxidative activity of the known antioxidant ionol was unchanged.


Assuntos
Antioxidantes/farmacologia , Hidroxitolueno Butilado/farmacologia , Fentolamina/farmacologia , Ácido gama-Aminobutírico/análogos & derivados , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Galinhas , Relação Dose-Resposta a Droga , Gema de Ovo , Medições Luminescentes , Masculino , Oxirredução/efeitos dos fármacos , Ratos , Ácido gama-Aminobutírico/farmacologia
3.
Farmakol Toksikol ; 53(5): 61-2, 1990.
Artigo em Russo | MEDLINE | ID: mdl-2253755

RESUMO

It was established on two age groups of rats that toxic brain edema in one-month-old animals is prevented by dopegit (100 mg/kg) and aminazine (2.5 mg/kg). The pharmacological correction of the brain edema in two-month-old rats is similar to that in adult animals. The central adrenergic structures play the significant role in the development of the brain edema in sexually immature animals.


Assuntos
Edema Encefálico/prevenção & controle , Sistema Nervoso/efeitos dos fármacos , Maturidade Sexual/efeitos dos fármacos , Envelhecimento/efeitos dos fármacos , Animais , Edema Encefálico/induzido quimicamente , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Nicotina , Ratos
4.
Farmakol Toksikol ; 52(4): 37-9, 1989.
Artigo em Russo | MEDLINE | ID: mdl-2806525

RESUMO

In experiments on rats it was found that fenibut (50 mg/kg, 1/20 of LD50) during a single and repeated administration in the fetus period of pregnancy does not exert any negative effect on the maternal organism, the growth and development of the fetus. Seduxen administered in a dose of 50 mg/kg (1/80 of LD50) alone and in combination with fenibut was shown to decrease the female body weight gain and to disturb the fetus development. Following a single administration on the 17th day of pregnancy, the effect was poorly pronounced.


Assuntos
Diazepam/efeitos adversos , Desenvolvimento Embrionário e Fetal/efeitos dos fármacos , Prenhez/efeitos dos fármacos , Tranquilizantes/efeitos adversos , Ácido gama-Aminobutírico/análogos & derivados , Animais , Peso Corporal/efeitos dos fármacos , Feminino , Idade Gestacional , Osteogênese/efeitos dos fármacos , Gravidez , Ratos , Ácido gama-Aminobutírico/efeitos adversos
5.
Farmakol Toksikol ; 51(4): 62-3, 1988.
Artigo em Russo | MEDLINE | ID: mdl-3191975

RESUMO

In chronic experiments on female rabbits it was shown that GABA-receptor agonist phenibut given in small doses exerts the stimulating effect, while GABA and phenibut administered in large doses suppress the uterine contractile activity, acting probably as modulators of presynaptic release of neuromediators. Diazepam displays the regulatory effect on the uterine contractions via the postsynaptic receptor mechanisms. The data suggest the involvement of the GABAergic mechanisms in the uterine contractile function.


Assuntos
Contração Uterina/efeitos dos fármacos , Ácido gama-Aminobutírico/metabolismo , Animais , Diazepam/farmacologia , Relação Dose-Resposta a Droga , Feminino , Coelhos , Fatores de Tempo , Ácido gama-Aminobutírico/análogos & derivados , Ácido gama-Aminobutírico/farmacologia
6.
Farmakol Toksikol ; 50(2): 91-3, 1987.
Artigo em Russo | MEDLINE | ID: mdl-3582643

RESUMO

It was shown in experiments on rats on models of toxic and traumatic edemas-swellings that etimizol (5 and 1 mg/kg) prevented changes in total content of water and the cerebral tissue density.


Assuntos
Edema Encefálico/tratamento farmacológico , Etimizol/uso terapêutico , Imidazóis/uso terapêutico , Adrenalectomia , Animais , Água Corporal/efeitos dos fármacos , Edema Encefálico/etiologia , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Ratos , Fatores de Tempo
7.
Biull Eksp Biol Med ; 100(11): 576-8, 1985 Nov.
Artigo em Russo | MEDLINE | ID: mdl-2998506

RESUMO

Experiments on isolated strips of the rabbit uterus showed the ability of GABA, GABAA-receptor agonist (diazepam) and GABAB-receptor antagonist (phenibut) to inhibit uterine contractility. GABAA-receptor antagonist (bicuculline) had a stimulating effect on contractility. It is assumed that GABA-ergic system plays an important role in the regulation of functional inhibition of contractile activity in the rabbit uterus, with GABA agonists regarded as potential gravidoprotectors in uterine hyperactivity or threatening miscarriage.


Assuntos
Diazepam/farmacologia , Músculo Liso/efeitos dos fármacos , Receptores de GABA-A/efeitos dos fármacos , Ácido gama-Aminobutírico/análogos & derivados , Ácido gama-Aminobutírico/farmacologia , Animais , Bicuculina/farmacologia , Convulsivantes/farmacologia , Feminino , Técnicas In Vitro , Contração Muscular/efeitos dos fármacos , Coelhos , Útero/efeitos dos fármacos
10.
Farmakol Toksikol ; 48(3): 77-9, 1985.
Artigo em Russo | MEDLINE | ID: mdl-2993020

RESUMO

Thirty-three experiments were made on mongrel dogs operated on according to Basov, with the use of phentolamine, pilocarpine, atropine, histamine and their combinations. It was established that administration of histamine gives rise to an increase in gastric secretion, provided the animals are pretreated with phentolamine or with combined pilocarpine and phentolamine. Histamine-induced gastric secretion considerably decreases, provided the animals are pretreated with atropine and ceases almost completely after administration of combined atropine and phentolamine. It is concluded that the stimulating effect of phentolamine on gastric secretion is caused by an increase in the sensitivity of H2-receptors and cholinoreceptors under blockade of the alpha-adrenoreactive systems.


Assuntos
Mucosa Gástrica/efeitos dos fármacos , Fentolamina/farmacologia , Animais , Atropina/farmacologia , Cães , Mucosa Gástrica/metabolismo , Histamina/farmacologia , Pilocarpina/farmacologia , Tempo de Reação/efeitos dos fármacos , Receptores Adrenérgicos alfa/efeitos dos fármacos , Receptores Histamínicos H2/efeitos dos fármacos
11.
Farmakol Toksikol ; 48(2): 18-21, 1985.
Artigo em Russo | MEDLINE | ID: mdl-2860007

RESUMO

Experiments on rats with experimental brain edema under water intoxication were made to study the effects of the neuroleptics aminazine and propazine, the central M-cholinoblocker amizyl and the alpha-adrenoblocker phentolamine on the time-course of the recovery of cortical electric activity after passing of the wave of Leao's spreading depression (SD). The drugs under study were demonstrated to have antiedematous properties under water intoxication and to make to a considerable degree for disorders in the processes of the recovery of cortical electrogenesis after SD. It is assumed that the action of the drugs on the electrophysiological parameters under study is associated with their effects on metabolic processes and with the presence of antiedematous properties.


Assuntos
Antipsicóticos/uso terapêutico , Benactizina/uso terapêutico , Edema Encefálico/tratamento farmacológico , Córtex Cerebral/efeitos dos fármacos , Clorpromazina/uso terapêutico , Parassimpatolíticos/uso terapêutico , Fentolamina/uso terapêutico , Triazinas/uso terapêutico , Animais , Edema Encefálico/fisiopatologia , Córtex Cerebral/fisiopatologia , Depressão Alastrante da Atividade Elétrica Cortical/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Potenciais Evocados/efeitos dos fármacos , Feminino , Masculino , Ratos
13.
Biull Eksp Biol Med ; 99(1): 67-9, 1985 Jan.
Artigo em Russo | MEDLINE | ID: mdl-2857099

RESUMO

It has been shown in rats with experimental toxic and traumatic edemas that picrotoxin (1 mg/kg) removes the antiedematous action of diazepam, phenazepam, phenibut and amizyl and reduces the action of phentolamine. When the dose of picrotoxin is minimized to 0.5 mg/kg such an effect is not observed. Prolonged daily administration of picrotoxin in a dose of 1 mg/kg results in the development of brain edema. It is recommended that GABA-positive drugs be included into a complex of treatment measures for edema.


Assuntos
Benzodiazepinas , Edema Encefálico/etiologia , Receptores de GABA-A/efeitos dos fármacos , Animais , Ansiolíticos/uso terapêutico , Benactizina/uso terapêutico , Benzodiazepinonas , Edema Encefálico/tratamento farmacológico , Lesões Encefálicas/complicações , Diazepam/uso terapêutico , Avaliação Pré-Clínica de Medicamentos , Interações Medicamentosas , Feminino , Masculino , Nicotina/toxicidade , Parassimpatolíticos/uso terapêutico , Fentolamina/uso terapêutico , Picrotoxina/farmacologia , Ratos , Ácido gama-Aminobutírico/análogos & derivados , Ácido gama-Aminobutírico/uso terapêutico
14.
Farmakol Toksikol ; 47(5): 47-50, 1984.
Artigo em Russo | MEDLINE | ID: mdl-6500034

RESUMO

Chronic experiments on ovariectomized rabbits were made to study the effect of sodium hydroxybutyrate, a gamma-hydroxybutyric acid derivative, on the myometrium. The mechanical distension of the uterine horn provoked hyperactivity. The dopamine agonist levodopa dramatically potentiated the mechanical hyperactivity of the rabbit uterus. Sodium hydroxybutyrate (800 mg/kg i.v.) significantly inhibited the mechanical and levodopa uterine hyperactivity. The most powerful inhibitory action was produced on the levodopa hyperactivity. Sodium hydroxybutyrate can be regarded as a potential gravidoprotector. It may be assumed that the dopaminergic system is involved in the development of the myometrium hyperactivity. The GABA-ergic mechanisms are likely to play a definite role in the reduction of uterine contractility.


Assuntos
Hidroxibutiratos/farmacologia , Oxibato de Sódio/farmacologia , Contração Uterina/efeitos dos fármacos , Animais , Castração , Depressão Química , Feminino , Levodopa/farmacologia , Tono Muscular/efeitos dos fármacos , Coelhos
15.
Farmakol Toksikol ; 47(3): 35-8, 1984.
Artigo em Russo | MEDLINE | ID: mdl-6145621

RESUMO

The development of toxic and traumatic brain edema in rats is accompanied by a decrease in the ATP level, in the total amount of adenyl nucleotides, the magnitude of the energy charge in the ATP-ADP-AMP system, and by an elevation in the content of AMP. Diazepam (0.5 mg/kg) and phenibut (50 mg/kg) that exert an antiedematous action reduce the amplitude of bioenergetic shifts during edema. As for piracetam (1000 mg/kg) it exhibits an insignificant effect. It is assumed that positive action of diazepam and phenibut on brain bioenergetics in edema is realized via the GABA-ergic system.


Assuntos
Ansiolíticos/uso terapêutico , Edema Encefálico/tratamento farmacológico , Encéfalo/efeitos dos fármacos , Metabolismo Energético/efeitos dos fármacos , Ácido gama-Aminobutírico/análogos & derivados , Animais , Benzodiazepinas , Encéfalo/metabolismo , Edema Encefálico/metabolismo , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Ratos , Fatores de Tempo , Ácido gama-Aminobutírico/uso terapêutico
17.
Farmakol Toksikol ; 47(1): 34-7, 1984.
Artigo em Russo | MEDLINE | ID: mdl-6142833

RESUMO

Experiments on rats were made to study the action of the derivatives of benzodiazepine (diazepam, 0.5 mg/kg and phenazepam, 0.1 mg/kg), and GABA (phenibut, 50 mg/kg, pantogam, 160 mg/kg, nicotinoyl-GABA, 500 mg/kg, piracetam, 1000 mg/kg) on the development of a traumatic brain edema. Diazepam, phenazepam and phenibut were demonstrated to produce a marked antiedematous action. The drugs made water content in the brain return to normal and reduced marked biochemical alterations in the brain. It is suggested that the protective action of the drug under study on the development of brain edema is linked with the action on the mediator structures and brain tissue metabolism.


Assuntos
Ansiolíticos/administração & dosagem , Edema Encefálico/tratamento farmacológico , Lesões Encefálicas/tratamento farmacológico , Ácido gama-Aminobutírico/análogos & derivados , Animais , Benzodiazepinas , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Edema Encefálico/metabolismo , Edema Encefálico/prevenção & controle , Lesões Encefálicas/complicações , Lesões Encefálicas/metabolismo , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Ratos , Ácido gama-Aminobutírico/administração & dosagem
18.
Farmakol Toksikol ; 46(6): 12-4, 1983.
Artigo em Russo | MEDLINE | ID: mdl-6140184

RESUMO

Experiments on rats with brain edema under water intoxication were made to examine the effect of the benzodiazepine tranquilizers diazepam and phenazepam on the time course of the recovery of brain electrical activity after passing the spreading Leao's depression wave. It was found that the drugs indicated possess antiedematous properties and improve brain function under these conditions. It is assumed that the drug action on the spreading depression is linked with their effect on metabolic processes in the brain and antiedematous properties.


Assuntos
Ansiolíticos/uso terapêutico , Benzodiazepinas , Benzodiazepinonas/uso terapêutico , Edema Encefálico/tratamento farmacológico , Depressão Alastrante da Atividade Elétrica Cortical/efeitos dos fármacos , Diazepam/uso terapêutico , Animais , Edema Encefálico/fisiopatologia , Avaliação Pré-Clínica de Medicamentos , Estimulação Elétrica , Eletroencefalografia , Potenciais Somatossensoriais Evocados/efeitos dos fármacos , Feminino , Masculino , Ratos , Intoxicação por Água/tratamento farmacológico , Intoxicação por Água/fisiopatologia
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