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1.
Farmakol Toksikol ; 53(3): 52-4, 1990.
Article in Russian | MEDLINE | ID: mdl-1974866

ABSTRACT

The comparative study of the psychotropic activity of new acyl derivatives of dibenzazepine and phenothiazine--bonnecor (chlorhydrate 3-carbethoxyamino-5(dimethylaminoacetyl) dibenzazepine and ethacizine (chlorhydrate 2-carbethoxyamino-10-(beta-diethyl-aminopropionyl)phenothiazine)--in the experiments on small laboratory animals showed the presence of the antidepressive, anxiolytic, antiamnesic and antihypoxic effects. The drugs exerted the psychotropic effects at administration in the doses exceeding those which influence the cardiovascular system. By the degree of the anxiolytic action bonnecor and ethacizine are inferior to diazepam, are as potent as trioxasine and are superior to meprobamat. The noted psychotropic action by its character and degree can serve as a beneficial supplement to the spectrum of the pharmacological activity of the studied compounds.


Subject(s)
Dibenzazepines/pharmacology , Phenothiazines/pharmacology , Psychotropic Drugs/pharmacology , Amnesia/drug therapy , Animals , Anti-Anxiety Agents , Anti-Arrhythmia Agents/pharmacology , Antidepressive Agents , Dose-Response Relationship, Drug , Hypoxia/drug therapy , Male , Mice , Rats , Structure-Activity Relationship
2.
Farmakol Toksikol ; 42(1): 76-81, 1979.
Article in Russian | MEDLINE | ID: mdl-570515

ABSTRACT

An experimental study of pyracetam (2-pyrrolidonacetamide) showed it capable to mitigate some behavioral and toxic manifestations of the action exerted by alcohol in tests on mice and rats, such as those of the "open field", "conflict situation", "rotating rod" and righting reflex. Pyracetam also attenuated some toxic symptoms of acetaldehyde in mice. It shortened the duration of coma, lessened the intensity of convulsive seizures, but it had no influence on the lethal effect of acetaldehyde. The type of the relation between doses and effects suggests the observed antagonism to be of a nonspecific nature.


Subject(s)
Acetaldehyde/poisoning , Alcoholic Intoxication/drug therapy , Piracetam/therapeutic use , Pyrrolidinones/therapeutic use , Acetaldehyde/antagonists & inhibitors , Alcoholic Intoxication/complications , Animals , Coma/drug therapy , Coma/etiology , Ethanol/antagonists & inhibitors , Humans , Mice , Movement Disorders/drug therapy , Movement Disorders/etiology , Rats , Seizures/chemically induced , Seizures/drug therapy , Substance Withdrawal Syndrome/drug therapy
3.
Farmakol Toksikol ; 39(6): 651-5, 1976.
Article in Russian | MEDLINE | ID: mdl-1088263

ABSTRACT

The spectrum of the psychotropic activity of a number of new pyrimidoindole derivatives and the relation between their chemical structure and activity were studied experimentally. The research was done on mice by employing tests usually applied in estimating neuroleptics and antidepressants of tricyclic structure. The study of indole derivatives are shown to display a sedative action. 5-methyl derivatives of pyrimido- and tetrahydropyrimido [3,4-a] indole without any substituent in the 2nd position are 5-oxytryptophan antagonists. The 2,5-dimethyltetrahydropyrimido [3,4-a] indole derivatives electively potentiate the central effect of 5-oxytryptophan and display in experiments a specific spectrum of the pharmacological action, resembling antidepressants by a number of tests. As concerns their activity these compounds, however, are inferior to amitriptyline and pyrasidol.


Subject(s)
Antidepressive Agents , Hypnotics and Sedatives , Indoles/pharmacology , Pyrimidines/pharmacology , Tranquilizing Agents , 5-Hydroxytryptophan/antagonists & inhibitors , Amphetamine/antagonists & inhibitors , Animals , Behavior, Animal/drug effects , Chemical Phenomena , Chemistry , Drug Synergism , Humans , Hyperkinesis/chemically induced , Hyperkinesis/drug therapy , Indoles/therapeutic use , Mice
4.
Farmakol Toksikol ; 39(4): 407-11, 1976.
Article in Russian | MEDLINE | ID: mdl-1036166

ABSTRACT

Following introduction of triftazine (2 mg/kg) and phthoracizine 8 mg/kg, separately and in combination, the intensity of catalepsy, the content of dopamine, norepinephrine (fluorometrically), of acetylcholine (biologically) and the activity of cholinesterase (calorimetrically) in the caudate nuclei and the frontal part of the cortex were determined in rats. It was established that with its one-time administration phthoracizine, while keeping down the intensity of triftazine-induced catalepsy, prevents, at the same time, the development of a number of biochemical effects, viz. there appears a distinctly pronounced tendency toward mormalization of the dopamine, acetylcholine levels and of the cholinesterase activity. A multiple joint administration of the drugs is also attended by lowering the intensity of catalepsy. Then, biochemical changes manifest themselves in more complex interrelations.


Subject(s)
Catalepsy/drug therapy , Parasympatholytics/therapeutic use , Phenothiazines/therapeutic use , Trifluoperazine , Acetylcholine/metabolism , Animals , Catalepsy/chemically induced , Catalepsy/metabolism , Caudate Nucleus/drug effects , Caudate Nucleus/metabolism , Cholinesterases/metabolism , Dopamine/metabolism , Drug Antagonism , Humans , Male , Norepinephrine/metabolism , Parasympatholytics/administration & dosage , Parasympatholytics/pharmacology , Phenothiazines/administration & dosage , Phenothiazines/pharmacology , Rats
5.
Article in Russian | MEDLINE | ID: mdl-944516

ABSTRACT

Catalepsy occurring in rats in a singular and repeated introduction of triftasine has a manifold mechanism, the main components of which are related to the metabolism of dophamine, acetylcholine and cholinesterase activity. A change in the intensity of catalepsy in a multiple introduction of the preparation is due mainly to cholinergic influences.


Subject(s)
Catalepsy/chemically induced , Caudate Nucleus/metabolism , Frontal Lobe/metabolism , Trifluoperazine , Acetylcholine/metabolism , Animals , Caudate Nucleus/enzymology , Cholinesterases/metabolism , Dopamine/metabolism , Epinephrine/metabolism , Frontal Lobe/enzymology , Humans , Male , Norepinephrine/metabolism , Rats
6.
Farmakol Toksikol ; 38(3): 277-81, 1975.
Article in Russian | MEDLINE | ID: mdl-1227900

ABSTRACT

Correlation between the dynamics of triftazine (stelazine, trifluoperazine) distribution in the brain, liver, and blood plasma of rats and the dynamics marking the development of cataleptic and antiagressive effects and also upset motor conditionation was studied. It was found that following oral administration of triftazine it slowly reaches the organs, the greatest part being adsorbed in the liver. On the contrary, of its intramuscular administration is characteristic a quicker accumulation in the organs and then the level of the neuroleptic in the brain and plasma is higher and in the liver - lower than with its oral introduction. A dissimilar dynamics of triftazine in the brain explains the difference of its pharmacological effects with diverse modes of administration. When given by mouth the content of the drug in the brain is insignificant and it rises but slowly, this being matched by a correspondingly slow development of the effects of triftazine. With the intramuscular route of introduction the neuroleptic's content in the brain rapidly reaches a high level, while its pharmacological effects are characterized by a quicker development than this is the case with its oral administration.


Subject(s)
Trifluoperazine/metabolism , Administration, Oral , Animals , Blood/metabolism , Brain/metabolism , Injections, Intramuscular , Kinetics , Liver/metabolism , Male , Rats , Time Factors , Trifluoperazine/administration & dosage , Trifluoperazine/pharmacology
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