[Gas chromatographic method for the quantitative determination of ftoratsizin and its N-dealkylated metabolites in animal and human biological material]. / Gazokhromatograficheskii metod kolichestvennogo opredeleniia ftoratsizina i ego N-dezalkilirovannykh metabolitov v biologicheskom materiale zhivotnykh i cheloveka.

Conditions have been selected, providing the most complete transformation of ftoracizin 10-(beta-diethylaminopropionyl)-2-trifluoromethylphenothiazine and its two dealkylated metabolites--deethylftoracizin 10-(beta-ethylaminopropionyl)-2-trifluoromethylphenothiazine and dediethylftoracizin 10-(beta-aminoprpiony 17-2-trifluoromethylphenothiazine to 10-akryloyl-2-trifluoromethylphenothiazine in the injector of a chromatograph. The detector for electrons 63Ni uptake was extremely sensitive to the above substance. A method has been developed for quantitative determination of ftoracizin, diethylftoracizin and dediethylftoracizin in animal and human bioloigcal material.

[Effect of piracetam on some manifestations of the effects of ethanol and acetaldehyde]. / Vliianie piratsetama na nekotorye proiavleniia deistviia etanola i atsetal'degida.

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.

[Effect of several psychotropic agents on changes in the behavior of mice induced by acetaldehyde]. / Vliianie nekotorykh psikhotropnykh sredstv na izmeneniia povedeniia myshei, vyzyvaemye atsetal'degidom.

Results of a study on the effect produced by 26 psychotropic agents on a complex set of behavioral changes in mice induced by introduction of acetaldehyde are presented. Experiments were conducted according to the method of Ortiz et al. (1973) who have proposed this test as a model of the abstinence syndrome. The effect of the agents was evaluated by removal of convulsions according to the Goldstein 4-point scale system (1972). In this respect the most effective proved tranquilizers, hypnotics, sodium oxybutyrate and ethanol. Little effective were neuroleptics and antidepressants. The model may be used in the screening of drugs when treating the abstinence syndromes in chronic alcoholism.

[Features of ethmozine metabolism]. / Osobennosti metabolizma étmozina

A study of the aethozine metabolism in the urine of rats detected 14 metabolites, a number of which was identified, namely: 2-aminophenothiazine, 2-acetylamide-phenothiazine, ethyl ether of phenothiazine-carbamine-2-acid, their sulphoxides and also aethmozine sulphoxide. Of the aethmozine biotransformation processes is characteristic formation in the organism of the animals of significant quantities of transformation products with complete degradation of the side chain.

[Pharmacologic activity of pyrimidoindole derivatives]. / Farmakologicheskaia aktivnost' proizvodnykh pirimidoindola

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.

[Neurochemical aspects of corrective effect of fluoracizine in triphthazine-induced catalepsy in rats]. / Neirokhimicheskie aspekty korrektornogo deistviia ftoratsizina pri triftazinovoi katalepsii u krys.

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.

[Elimination of products of fluoracizine by the gastrointestinal tract in animals of different species]. / Vyvedenie produktov prevrashcheniia ftoratsizina zheludochno-kishechnym traktom u zhivotnykh raznykh vidov

A study on elimination of phthoracizine metabolites with feces of different animal species evidenced that bulk of its transformation products with an intact side-chain was contained in the feces of rats. In the feces of mice they are found in much smaller amount, while in rabbits they are practically untracable. The phthoracizine transformation products devoid of the side-chain are demonstrable both in rats and in other animal species either as traces or not definable at all. These phenomena are, apparently, to be attributed to a different ability of eliminating the phthoracizine biotransformation products with bile by different animal species, which, among other factors. is determined by the molecular weight of individual metabolites.

[The effect of long-term nitrazepam administration on sleep cycles in rats]. / Vliianie dlitel'nogo vvedeniia nitrazepama na tsikly sna u krys

Single and chronic administration of a low dose of nitrazepam (1 mg/kg) had no effect on sleep cycles in rats. A single injection of a high dose (10 mg/kg) of nitrazepam resulted in prolongation of the total duration of synchronized sleep with a corresponding shortening of desynchronized (paradoxical) sleep. The number of sleep cycles was reduced. Chronic injections of nitrazepam (for 7-14 days) in a dose of 10 mg/kg evoked a gradual prolongation of the duration of paradoxical sleep and an increase in number of sleep cycles. After discontinuance of a long-term administration of nitrazepam (1 mg/kg or 10 mg/kg) prolongation of desynchronized sleep and an increase in the number of sleep cycles were more pronounced in comparison with the last day of chronic administration of the drug.

[The role of catecholamines, acetylcholine and cholinesterase activity in the development of the cataleptic action of triftazin following repeated administration]. / Rol' katekholaminov, atsetilkholina i aktivnosti kholinésterazy v razvitii katalepticheskogo deistviia triftazina pri ego mnogokratnom vvedenii

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.

[Comparative characteristics of fluorasizine metabolism in different species of animals and man]. / Sravnitel'naia kharakteristika metabolizma ftoratsizina u razlichnykh vidov zhivotnykh i cheloveka

The process of phthoracizine (10-(beta-diethylaminopropiniol)-2-triphthormethylphenothiazine hydrochloride) transformation proceeding in various animal species and in man is similar in grosso modo to biotransformation of chlorpromazine and of compounds related to the latter, including sulphoxidation, dealkylation in the side chain nitrogen, hydroxylation, glucoronoconjugation and the formation of products with the side chain degradation. At the same time, one can note a difference which finds its expression in the development of a large quantity of the phthoracizine metabolites attended by destruction of the side chain, as well as of hydroxylated sulphoxidated products of its transformation. In rats, more than in rabbits and mice, the spectrum of the phthoracizine metabolites is closer to the products of its biotransformation passed with the human urine.

[Correlation between the distribution of triftazin in certain organs of rats and its pharmacological effects when administered by different methods]. / O sootnoshenii mezhdu raspredeleniem triftazina v nekotorykh organakh krys i ego farmakologicheskimi éffektami pri raznykh sposobakh

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.