[The effect of adrenergic blocking substances on phenamine toxicity in grouped and isolated mice].
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Amphetamine↗
Biomedical subjects
K S Raevskiĭ
Publications and source records attributed to K S Raevskiĭ.
[A comparative assessment of the stimulatory effect of phenamine and pervitine when used simultaneously with a methyl group donor or acceptor].
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Amphetamine↗
[Pharmacokinetic study of the neuroleptic, azabutyrone].
By using gas-chromatographic and spectrophotometric assays and adopting pharmacokinetic models of various types the pharmacokinetics of the neuroleptic azabutyron in the plasms, bile, gastric juice and urine of rabbits and rats was studied. The maximum level of azabutyron in the plasma (27 gamma/ml) was recorded 5 minutes after introduction of the drug. The amount of unchanged azabutyron passed with urine comprises 2--4 pc of the dose actually introduced, while the quantity of the agent excreted together with the bile and gastric juice was below 1 pc. The results thus obtained were subjected to electronic data processing according to the two-compartment pharmacokinetic model. It is presumed that in order to properly explain the pharmacokinetics of azabutyron some models of a greater complexity have to be used.
Animals↗
[Liberation of H3-GABA from isolated nerve endings of the cerebral cortex of rats under the effect of psychotropic drugs].
The influence of a number of neuroleptics and antidepressants on the release of 3H-GABA from the synaptosomas of the cerebral cortex in rats was studied. Chlorpromazine, phthorphenazine, trifluperidol, imipramine, phthoracizine caused an intensified liberation of 3H-GABA from the synaptosomas. In this phenothiazine neuroleptics proved more active than did trifluperidol and antidepressants. New neuroleptics--azabuperon and carbidine and also diphenylhydantoin tended to restrict the liberation of the mediator from synaptosomas. The tranquilizer diazepam, gamma-oxybutyric acid and carbamazepine failed to have any significnat effect on this process. The described effects of thepsychotropic substances are due, apparently, to their direct influence on the synaptomal membrane.
Aminobutyrates↗
[The effect of anticonvulsants on the nitric oxide content and level of lipid peroxidation in the brain of rats in model seizure states].
EPR spectroscopy was performed to study the effect of anticonvulsants lamotrigine and phenobarbital on nitric oxide generation in rat brain on models of a convulsive seizure caused by exposure to maximal electric shock or corasole injection. The intensity of lipid peroxidation (LPO) was studied at the same time. The anticonvulsants under study proved to be capable of suppressing to a various degree intensification of nitric oxide generation and increase of LPO intensity in the rat cerebral cortex induced by convulsions. This widens the existing idea of the mechanism of the effect of antiepileptic agents.
Animals↗
[The effect of the dopamine neuronal reuptake inhibitor GBR 12909 on the dopaminergic neurotransmission parameters in the rat striatum in vivo].
The aim of the present research was to investigate the effects of the selective dopamine re-uptake inhibitor GBR 12909 (10 mg/kg, i.p.) on dopaminergic neurotransmission in rat striatum. GBR 12909 increased DA levels in microdialysis samples from freely moving rats. In contrast, administration of GBR 12909 slightly decreased the NSD 1015 (50 mg/kg)--induced DOPA accumulation. This result may be explained as a decrease in DA biosynthesis in response to an increasing amount of DA in the synaptic cleft. Fast-scan cyclic voltammetric monitoring of electrically-evoked DA showed significant changes after the drug in DA re-uptake (Km), but not DA release. In conclusion, our results support the notion, that GBR 12909 is a specific DA uptake inhibitor without any transmitter releasing action.
Animals↗
[Semax prevents elevation of nitric oxide generation caused by incomplete global ischemia in the rat brain].
A twofold increase in the nitric oxide (NO) production and a moderate increase in the content of secondary products of lipid peroxidation was observed in Wistar rats with incomplete global ischemia model induced by the bilateral occlusion of common carotid arteries. A clear correlation was observed between the NO content in the rat brain and the level of neurological disturbance manifestations in the ischemized animals. The synthetic peptide semax (a fragment of ACTH4-7 Pro-Gly-Pro) in a dose of 0.3 mg/kg prevented from the development of both neurological disturbances and excess NO production in the rat brain cortex.
Adrenocorticotropic Hormone↗
[Effect of psychotropic substances on the uptake of [H3]-gamma-aminobutyric acid by rat brain synaptosomes].
The in vitro effects of some neuroleptics and antidepressants on the accumulation of [3H]/-GABA by the synaprosomes of the rat brain cortex were studied. Chloropromazine, trifluoperazine, fluphenazine, perphenazine, thioproperazine, haloperidol, trifluperidol, droperidol, imipramine, haloanison and phthoracyzine were found (in order of a decreasing activity) to inhibit the [3H]/-GABA uptake of synaptosomes. Neuroleptics, except for a new drug carbidine, proved to be more potent inhibitors than antidepressants are. The tranquilized diazepan failed to have any effect on the [3H]/-GABA uptake. The rats synaptosomes treated with chlorpromazine and imipramine were found to display a decreased ability to accumulate [3H]/-GABA. The suppressive effect of psychotropic agents on the [3H]/-GABA uptake by synaptosomes is suggested to be due, at least partly, to their known inhibitory influence on the Na+, K+-dependent ATPase.
Aminobutyrates↗
[Behavioral analysis of consequences of chronic blockade of NMDA-type glutamate receptors in the early postnatal period in rats].
In view of the hypothesis that glutamatergic dysfunction of brain can underlie the negative symptoms of schizophrenia (including cognitive deficit), the aim of this study was to develop a model of cognitive impairment in Wistar male rats after administration of a noncompetitive NMDA-receptor antagonist in early postnatal period. Rat pups were daily subcutaneously injected with 0.05 mg/kg MK-801 on postnatal days 7-49. On the 27th and 28th days 24 h after the last previous injection, the MK-801-treated rats demonstrated lower spontaneous locomotor and exploratory activity in comparison with saline control, however, they retained the reaction of hyperlocomotion which developed immediately after the MK-801 administration. In these rats, the anxiety level in the elevated plus-maze (on the 40th postnatal day) was found to be decreased, and the spatial learning in food rewarded task was negatively affected (on the 50th-54th days). It is suggested that impairment of the input of sensory information and its correct assessment by the animals can be associated with the early neonatal blockade of NMDA glutamate receptors.
Animals↗
[Effect of the new potential anti-Parkinson agent, hymantane, on levels of monoamines and their metabolites in rat striatum (a microdialysis study)].
The new aminoadamantane derivative N-(2-adamantyl)hexamethyleneimine hydrochloride (A-7, hemantane) exhibited a pronounced antiparkinsonian effect on various experimental models. Hemantane showed a broad activity spectrum, being superior to amantadine (midantane) in some tests. Administered in an effective antiparkinsonian dose, hemantane increased the extracellular dopamine content in the striatum. The drug also produced a dose-dependent decrease in the extracellular level of dihydroxyphenylacetic acid and homovanillic acid (DOPAC and HVA, the dopamine metabolites) and 5-hydroxyindoloacetic acid (5-HIAc, a serotonin metabolite) in the striatum, which may reflect inhibition of the monoamine oxidase activity in the brain. These results show that the dopaminergic and serotoninergic nigrostriatial systems are involved in the mechanism of hemantane action.
Adamantane↗
[Effect of promedol and fentanyl on the permeability of the hemato-encephalic barrier of rats for noradrenaline-H3].
In tests situations with rats it was shown that promedol and phentanide produce an analgetic action accompanied by a reduced flow of tagged norepinephrine from the blood into the brain. A parallelism between the dosage of the substances and the intensity of the analgetic effect and the degree of changed permeability of the blood-cerebral barrier could be noted.
Animals↗
[Extracellular level of neuroactive amino acids in the rat neostriatum after treatment with psychostimulants (microdialysis study)].
The effects of acute and subchronic (four times with a 2-h interval) intraperitoneal administration of d-amphetamine and sydnocarb in equimolar doses (5 and 23.8 mg/kg, respectively) on the intracellular level of glutamate, asparate, taurine, and alanine in neostriatum of male Sprague-Dawley rats anesthetized with halothane was studied. It was shown that repeated introduction of the psychostimulants leads to a significant increase in the content of all four neuroactive amino acids in neostriatum dyalisates. However, the effects of sydnocarb were less pronounced as compared to those of d-amphetamine, which is indicative of a lower neurotoxic potential of the former drug and confirms a significant difference in the neurochemical mechanisms of action of the two drugs studied. The massive increase in the extracellular content of taurine probably reflects hyperactivation of the glutamatergic transmission in the neostriatum and may serve as a marker of neurotoxicity.
Animals↗
[Spectrophotometric determination of azabutyrone in biological material].
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Animals↗
[Locomotor activity and expression of c-Fos protein in the brain of C57BL and Balb/c mice: effects of D-amphetamine and sydnocarb].
Effects of the psychostimulants D-amphetamine and sydnocarb on the locomotor activity and c-Fos protein expression in the brain of C57BL and BALB/c mice was studied. The drugs significantly increase the locomotor activity and the level of c-Fos protein in the brain structures of both lines. The effect of D-amphetamine with respect to the locomotor activity was more pronounced in C57BL mice, which correlates with a higher level of the c-Fos expression in the secondary motor cortex. At the same time syndocarb more significantly than D-amphetamine induces expression of the c-Fos protein in the nucleus accumbens core of C57BL mice. Injection of an 0.85% NaCl solution led to a moderate increase in the locomotor activity in the mice of both lines, while the c-Fos expression in the secondary motor cortex and septum was more pronounced in C57BL than in BALB/c mice.
Animals↗
[Effect of 17beta-estradiol on haloperidol effects in Wistar rats].
It is established that the haloperidol catalepsy is much less pronounced in Wistar females than in males. Estradiol (10 mg/kg, i.p.) decreased intensity of the haloperidol catalepsy, reduced the haloperidol-induced increase in the dopamine turnover, and decreased the level of dopamine metabolites in nucleus accumbens of both female and male test animals. However, these effects are also more pronounced in females.
Animals↗
[Combined effect of amphetamine and midantan on the dopaminergic transmission in the striatum of freely moving rats].
The combined action of midantane (amantadine, a noncompetitive NMDA receptor antagonist used as an antiparkinsonian drug) and amphetamine (a psychostimulant) on the extracellular level of dopamine and its metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) was studied in the striatum of freely moving Wistar rats. After the administration of amphetamine (AMPH) in a dose of 10 mg/kg (i.p.), the extracellular level of dopamine exhibited a sharp increase in (up to 700% relative to the basal level) within 20-40 min and then gradually decreased. One hour after the injection of AMPH, the content of DOPAC and HVA decreased by 60 and 40%, respectively, and then was retained on this level. Midantane (20 mg/kg, i.p.) injected alone did not influence the level of dopamine and its metabolites. Administered together with AMPH, midantane prevented the extracellular accumulation of dopamine, but did not change the extracellular level of its metabolites reduced by AMPH. These results suggest that NMDA receptor antagonists can block the AMPH-stimulated dopamine release from a vesicular pool, while not affecting the other components of dopamine action such as the re-uptake reversal and inhibition of monoamine oxidase.
3,4-Dihydroxyphenylacetic Acid↗
[Antipsychotic agents: from phenothiazines to atypical neuroleptics of the second generation].
The paper addresses evolution of the problem of creation, characterization of the pharmacological properties, and elucidation of the mechanisms of action of antipsychotic drugs (neuroleptics)--one of the most important classes of modern psychotropic drugs. The appearance of these drugs marked the onset of a new era in psychiatry, the era of psychopharmacology. Special attention is devoted to the investigations in this direction at the Institute of Pharmacology, which were headed by V. V. Zakusov.
Antipsychotic Agents↗
[Effects of antagonists of the various subtypes of dopamine receptors on the locomotor activity of C57BL mice induced by psychostimulators].
The involvement of dopamine receptors of various subtypes in the mechanisms of locomotor hyperactivity caused by single administration of psychostimulants d-amphetamine and syndnocarb was studied in C57BL mice. Administered in a dose not influencing the spontaneous locomotor activity, SCH23390 and raclopride--selective antagonists of the D1 and D2 subtypes of dopamine receptors, respectively--abolished the hyperactivity induced by d-amphetamine, while not significantly changing the effect of sydnocarb. On the contrary, clozapine--antagonist of the D4 subtype of dopamine receptors--failed to reduce the stimulant action of d-amphetamine, but significantly decreased the effect of sydnocarb under the same experimental conditions.
Animals↗