[Effect of selective activation of central serotoninergic systems on the course of the early post-traumatic period]. / Vliianie selektivnoi aktivatsii tsentral'nykh serotoninergicheskikh sistem na techenie rannego post-travmaticheskogo perioda.

The central administration of the serotonin agonists of receptors type 1A (Campiron) and type 2 (1-(2,4,5-trimethoxy)-2-aminopropanome) was experimentally demonstrated to cause a significant decrease in mortality rates and cardiovascular disorders in white rats traumatized according to Kennon. This effect was realized by maximally activating the hypothalamo-neurohypophysis, hypothalamo-hypophysis-adrenocortical systems and blocking activation of the hypothalamo-hypophysis-thyroidal system.

[Effect of selective activation and blockade of the central dopaminergic system on the course of the early post-traumatic period]. / Vliianie selektivnoi aktivatsii i blokady tsentral'nykh dofaminergicheskikh sistem na techenie rannego posttravmaticheskogo perioda.

Acute experiments on white rats traumatized according to Kenon demonstrated that the central administration of the dopamine receptor agonist apomorphine led a reduction in mortality rates and an increase in stroke and heart indices. The latter was due to the significant activation of the hypothalamo-hypophysis-thyroidal system. The use of sulpiride as a specific dopamine receptor blocker increased mortality rates and decreased stroke and heart indices. This was accompanied by the maximum activation of the hypothalamo-neurohypophyseal system.

[Nootropic substances enhance the N-methyl-D-aspartate-induced short-term potentiation of synaptic transmission in rat hippocampal slices]. / Nootropnye veshchestva usilivaiut vyzyvaemuiu N-metil-D-aspartatom kratkosrochnuiu potentsiatsiiu sinapticheskoi peredachi v srezakh gippokampa krys.

The nootropic agents pyracetam, ethymisole, N-5-oxynicotinoyl glutamate and beta-carboline derivative--ambocarb--enhance short-term potentiation of populational EPSP's amplitude of area CA1 pyramidal neurons in the slices of the rat hippocampus, which is evoked by NMDA. The inhibitors of protein kinases diminish the effect of pyracetam and ethymisole (tolbutamide), as well as all the studied nootropic drugs (polymyxin B and trifluoroperazine).

[The different mechanism of the inhibition by buspirone and its camphorimide analogs of 5-HT3-serotoninergic effects]. / Raznyi mekhanizm ingibirovaniia buspironom i ego kamforimidnymi analogami 5-HT3-serotoninergicheskikh éffektov.

Serotonin evokes the depolarization and the membrane resistance lowering of rat dorsal root ganglion neurones when a K(+)--conductance of the neuronal membranes is blocked by Cs+ intracellular injection. These 5-HT3-effects ere diminished and removed by preliminary superfusion of the ganglions with saline containing busperone or its structural analogues. The effects of camphorimide analogues of buspirone (campirone, pyricapirone) could not be reproduced in case of the protein kinase A blockade by tolbutamide (100 microM/l). It is suggested that camphorimide analogues are the 5-HT3 receptor blockers while busperone and ipsapirone modulate 5-HT3 receptor affinity by decreasing the protein kinase A activity.

[Lithium ion modulation of the neuronal responses evoked by monoaminergic receptor agonists]. / Moduliatsiia ionami litiia otvetov neironov, vyzyvaemykh agonistami monoaminergicheskikh retseptorov.

The authors studied the action of lithium ions on the responses of rat dorsal root ganglion neurons and frog spinal motoneurons evoked by monoamine agonists using the microelectrode technique. Lithium ions reversibly inhibit the depolarizing responses of spinal sensory neurons and motoneurons evoked by activation of muscarinic choline-, alpha 1-adreno-, and 5-hydroxytryptamine2 receptors, but enhance the hyperpolarizing neuronal responses evoked by activation of 5-hidroxytryptamine1A receptors.

[Nootropic drugs potentiate nerve cell responses evoked by NMDA-glutamate receptor activation]. / Nootropy potentsiruiut otvety nervnykh kletok, vyzyvaemye aktivatsiei NMDA-glutamatnykh retseptorov.

The nootropic drugs--nootropil, aethimizol, diethylaminoethanol, and ambocarb diminished of amnesia of active avoidance habit evoked by maximal electroconvulsive shock in the rats. At the same time tested nootropic drugs potentiated the frog spinal motoneurons responses mediated by NMDA, but not non NMDA glutamate receptors activation. It was discussed the role of NMDA-potentiating nootropic drugs action in their anti-amnestic action.

[The GABA-ergic component of the anxiolytic action of 1-(2-pyrimidinyl)-piperazine derivatives]. / GAMKergicheskii komponent anksioliticheskogo deistviia proizvodnykh 1-(2-pirimidinil)-piperazina.

The 1-(2-pyrimidinyl)-piperazine derivatives campirone, campironine, levopironine) evoked hyperpolarizing responses of rat dorsal root ganglion neurons mediated by 5-hydroxytryptamine(1A) receptor activation and, like chlordiazepoxide, potentiated neuronal responses evoked by GABA-depolarizing receptor activation. The drugs studied in the lighted space and threatening situation avoidance tests showed an anxiolytic effect. Picrotoxin was found to be effective in inhibiting the anxiolytic effect of chlordiazepoxide, levopironine and campironine, but it failed to affect the antianxious action of campirone. Whether the GABA-ergic mechanisms may contribute to the anxiolytic action of 1-(2-pyrimidinyl)-piperazine derivatives.

[The serotonin- and dopaminergic mechanisms in the action of 1-pyrimidinyl piperazine derivatives]. / Serotonin- i dofaminergicheskie mekhanizmy v deistvii proizvodnykh 1-pirimidinil-piperazina.

It has been established in experiments on spinal ganglia neurons of rats that 1-pyrimidinyl-piperazine derivatives show the properties of partial agonists of 5-HT1A-receptors. Some of them were discovered to be capable of blocking D2-dopamine receptors. Comparison of neuronal and behavioral activity of the substances tested has demonstrated that their anxiolytic activity detectable under the conditions of the conflict situation method significantly correlates with 5-HT1A-mimetic and anti-dopamine activity. The latter one correlates well with the influence of the substances tested on the time of immobilization in the forced swimming test.

[Effect of monoamines on the responses of frog spinal motor neurons mediated by non-NMDA glutamate receptors]. / Vliianie monoaminov na otvety motoneironov spinnogo mozga liagushek, oposreduemye neNMDA-glutamatnymi retseptorami.

Adrenaline, dopamine and 5-hydroxytryptamine enhanced fast desensitizing responses of frog spinal motoneurons evoked by L-glutamic acid. Monoamines also enhanced late components of dorsal root EPSP's of motoneurons. These effects of monoamines were prevented by ketamine. Slow in desensitizing responses evoked by L-glutamic acid and EPSP's of motoneurons evoked by stimulation of the reticular formation were not influenced by monoamines.

[The characteristics of the anxiolytic action of benzodiazepine and non-benzodiazepine tranquilizers in different tests of anxiety]. / Osobennosti anksioliticheskogo deistviia benzodiazepinovykh i nebenzodiazepinovykh trankvilizatorov na razlichnykh testakh trevogi.

In experiments on rats the presence or absence was studied of the phenomenon of potentiation of anxiolytic action, estimated by the time of the animal stay in the light part of the chamber in tests of avoidance of "the lighted ground" or "menacing situation" at combined application of the pairs of substances of benzodiasepine and non-benzodiasepine series (elenium, indoter, campiron and campironin). Spectra of their neurochemical activity were determined in experiments on neurones of isolated spinal ganglia of rats with intracellular biopotentials records. It has been established that GABA-potentiating action of indoter and elenium, dopamine-negative action of campiron and campironin are significant in their anxiolytic action in the states of alarm of aversive genesis of different modalities. Serotoninmimetic effect of non-diasepine tranquilizers is of functional significance in the test of avoidance of "the lighted ground", but not of the "menacing situation". It is suggested that differences of neurochemical mechanisms of anxiolytic action of the tested tranquilizers testify to different neurochemical profiles of the neuronal "matrices" of the studied states of alarm.

[Effects of serotonin-IA receptors on amino acid and dopaminergic responses of neurons]. / Vliianie agonistov serotoninovykh-IA retseptorov na aminoatsid- i dofaminergicheskie otvety neironov.

By using intracellular technique the authors studied the responses of frog spinal motoneurones and rat dorsal root ganglion evoked by GABA, L-aspartate and dopamine in the presence of 5-hydroxytryptamine and its 1A-agonists or without them. It is shown that buspirone, campirone and serotonin increase the GABA effects but inhibit the effects of aspartate via the GABA- and NMDA-receptors modulation.

Analysis of two types of dopaminergic responses of neurons of the spinal ganglia of rats.

It was established, in experiments on isolated spinal ganglia of adult rats in conditions of intracellular recording, that dopamine (1 microM/liter) elicits depolarized responses in 61% of neurons, hyperpolarized in 20% of neurons, and depolarized-hyperpolarized in 19% of neurons. The depolarized responses are associated with the activation of D1 dopamine receptors, and are governed by the shift of cAMP-dependent cation (sodium) channels to the conducting state. The hyperpolarized responses are triggered by the activation of D2 dopamine receptors, which by means of HTP-binding protein convert the potassium channels to the conducting state. The change in the polarization of neurons with the action of dopamine influences their electrical excitability variously.

[Reciprocal modulating effect of serotonin and dopamine on neurons of rat spinal ganglia]. / Vzaimnoe moduliruiushchee vliianie serotonina i dofamina pri ikh vozdeistvii na neirony spinal'nykh gangliev krys.

It was found in experiments on isolated dorsal root ganglion neurons of rats that dopamine (10(-8)-10(-6) Mol/l) potentiated depolarizing neuronal responses evoked by injection of 5-hydroxytryptamine from micropipette. Similar concentrations of 5-hydroxytryptamine (10(-8)-10(-6) Mol/l) potentiated neuronal depolarizing responses evoked by dopamine. Potentiating action of monoamines on combined neuronal responses depended on concentration and was inhibited by antagonists of dopamine (haloperidol) and 5-hydroxytryptamine (deseril) receptors. This effect of monoamines had postsynaptic nature and was bound with an increase of Ca2+ and cAMP intracellular concentrations.

[Postsynaptic metabolic monoamine modulation of effects mediated by NMDA glutamate receptors in spinal motoneurons of the frog]. / Postsinapticheskaia metabolicheskaia moduliatsiia monoaminami éffektov, oposreduemykh NMDA-glutamatnymi retseptorami, v spinal'nykh motoneironakh liagushek.

Monoamines, their agonists and antagonists have been investigated for their influence on responses of spinal motoneurons in frog mediated by NMDA-glutamate receptors (late components of dorsal root polysynaptic EPSP's and depolarizing responses evoked by L-aspartate). Monoamine responses which promoted an increase of intracellular concentration of cAMP and Ca2+ in the motoneurons (activation of alpha- and beta-adrenoreceptors, D1-dopamine and 5-hydroxytryptamine-receptors) reinforced the studied spinal motoneuron responses of frog. These responses were weakened by the monoamine action which led to a decrease of the intracellular concentration of cAMP and Ca2+ (activation of D2-dopamine and 5-hydroxytryptamine1A-receptors). The monoamine effects were inhibited by specific monoamine antagonists, tolbutamide and trifluoperazine. It is supposed that NMDA receptor-channel complex is exposed by cAMP- and Ca(2+)-calmodulin-dependent phosphorylation induced by activation of membrane monoamine receptors.

[The correlation of the serotonin-positive and anxiolytic activities of nonbenzodiazepine substances]. / Korreliatsiia serotoninpozitivnoi i anksioliticheskoi aktivnosti nebenzodiazepinovykh veshchestv.

The anxiolytic activity of serotonin agonists (buspirone, ipsapirone, campirone, caplapirone, 1-pyrimidinyl-piperazine) determined in rats on 3 experimental models of anxiety closely correlates with the degree of inhibition of impulse release of 3H-serotonin by electrically stimulated slices of the midbrain raphe dorsal nucleus (r = +0.85) but not the slices of the cerebral hemispheric cortex (r = +0.60) of the rats. The anxiolytic activity of neuroleptics (chlorpromazine, trifluorperazine), antidepressant (amitriptyline, imipramine) and beta-carbolines (harmane, 3.4-tetramethyleneharmane) corresponds well (r = +0.94) to the ability of the drugs to potentiate the hyperpolarizing effects of serotonin in the rat sensory ganglion.