Anxiolytic and Antidepressant Effects of Divaza and Brizantin.

The anxiolytic and antidepressant activities of complex preparations divaza and brizantin containing antibodies to brain-specific protein S100 were estimated using Vogel conflict test and Nomura forced swimming test. Course treatment (5 days) of brizantin in a dose of 2.5 ml/kg and divaza in a dose of 7.

Antidepressant Effect of Dimeric Dipeptide GSB-106, an Original Low-Molecular-Weight Mimetic of BDNF.

A large amount of clinical and experimental data suggest the involvement of neurotrophins, in particular the brain-derived neurotrophic factor (BDNF), in depression pathogenesis. However, the therapeutic use of BDNF is limited because of its instability in biological fluids, poor blood-brain barrier (BBB) permeability, and the presence of side effects. A low-molecular-weight mimetic GSB-106, which is a substituted dimeric dipeptide bis(N-monosuccinyl-L-seryl-L-lysine)hexamethylenediamide, was designed and synthesized based on the BDNF fourth loop structure at the V.

[Behavioral and neurochemical aspects of the antidepressive action of GSB-106 dipeptide BDNF fragment].

The behavioral and neurochemical effects of synthetic dipeptide fragment GSB-106 of BDNF, administered in a single dose of 0.1 mg/kg (i.p.

Anxiolytic activity of tenoten and diazepam depends on conditions in Vogel conflict test.

We compared two modifications of Vogel conflict test and assessed anxyolitic activity of two drugs: diazepam (benzodiazepine anxiolitic) and tenoten (ultra-low doses of antibodies to S-100 protein) in both modifications of the test. It was found that the intensity of anxiolitic effect of the drugs depends on the conditions of Vogel test.

[A drug with the broad spectrum of pharmacological activity for the treatment of complex neuropsychic disorders].

The influence of a pyrrolo-pyrazine derivative AL-613 (synthesized at the Zakusov Institute of Pharmacology) on the behavior of outbred male albino rats has been studied on various experimental models. It was established that AL-613 produces anxiolytic action in a conflict situation model and antidepressant action in forced swim paradigm test, improves active avoidance conditioned reflex acquisition, and increases the amplitude of transcallosal evoked potential. The substance demonstrated properties of anxiolytics, antidepressants, and nootropes.

[Effects of amitriptyline, fluoxetine, and tianeptine on the content of monoamines and their metabolites in Wistar rat brain structures].

The effects of antidepressant drugs belonging to different pharmacological groups--amitriptyline, fluoxetine (prozac), and tianeptine (coaxyl)--on the content of monoamines and their metabolites in Wistar rat brain structures (frontal cortex, hypothalamus, nucleus accumbens, striatum, and hippocamp) has been studied using HPLC with electrochemical detection. Tricyclic antidepressant amitriptyline (10 mg/kg) was found to produce a moderate increase in the DOPAC/dopamine turnover index in nucleus accumbens, but did not influence the levels of serotonin (5-HT), dopamine, and its metabolites (5-HIAA, DOPAC, and HVA) in other brain structures studied (frontal cortex, hypothalamus, striatum, hippocamp). Fluoxetine (Prozac) (20 mg/kg) decreased both the 5-HIAA content and the 5-HIAA/5-HT (5-HT turnover index) in all brain structures of Wistar rats.

Antiaggressive activity of antibodies to S-100 protein in ultralow doses.

Experiments on rats demonstrated antiaggressive activity of ultralow doses of antibodies to S-100 protein in tests of motivated and unmotivated aggression. The effect of ultralow doses of antibodies to S-100 protein in single and course treatment was not inferior to that of benzodiazepine anxiolytic diazepam.

Nootropic and antiamnestic effects of tenoten (pediatric formulation) in immature rat pups.

The antiamnestic effects of tenoten (pediatric formulation) was demonstrated on the model of scopolamine-induced amnesia of passive avoidance reflex and the nootropic effect of this preparation was demonstrated on the model of incomplete conditioning and in rat pups with experimental attention deficit syndrome. The efficiency of the preparation was comparable to that of piracetam and phenibut and even surpassed it by some parameters.

Comparison of antidepressant effects of azafan, tianeptine, and paroxetine.

Antidepressant activity of Russian product Azafen (pipofezine) and foreign products Paroxetine and Tianepine was compared using behavioral despair test (Porsolt test) and forced swimming test in a container with wheels (Nomura). Azafen significantly shortened the duration of depressive state in both tests. The results suggest that Azafen exhibits pronounced antidepressant activity, superior to that of the reference drugs.

[Effect of phenibut on interhemispheric transmission in the rat brain].

Effects of the nootropic drug phenibut on the transcallosal potential amplitude in the sensomotor brain cortex have been studied in rats. It is established that a single administration of phenibut in a dose of 25 mg/kg (i.p.

[Antidepressant properties of afobazole in Porsolt and Nomura tests].

Anxiolytic afobazole was shown in the experiments on outbred rats to decrease the immobility in the Porsolt and Nomura swim tests. The degree of afobazole effect in a dose of 5 mg/kg (i.p.

Involvement of the GABA-B system in the mechanism of action of ultralow-dose antibodies to S-100 protein.

The involvement of the GABA-B neurotransmitter system in the realization of anxiolytic and antidepressant activities of ultralow-dose antibodies to S-100 protein is demonstrated. Simultaneous injection of ultralow-dose antibodies to S-100 protein and GABA-B receptor agonist baclofen reduced the anxiolytic and antidepressant effects of the drug, while GABA-B receptor antagonist faclofen stimulated the anxiolytic and reduced the antidepressant effect of ultralow-dose antibodies to S-100 protein. The effect of ultralow-dose antibodies to S-100 protein on the GABA-B-ergic system differs from that of benzodiazepine anxiolytics (diazepam) and tricyclic antidepressants (amitryptiline) not affecting this transmitter system.

Anxiolytic and antidepressant characteristics of impaza.

Antibodies to endothelial NO synthase in ultralow doses exhibited anxiolytic and antidepressant effects and their efficiency after single and course treatment is not inferior to that of amitriptyline and diazepam. The psychotropic activity of ultralow-dose antibodies to endothelial NO-synthase is presumably one of important mechanisms of their efficiency in the treatment of erectile dysfunction.

[Mexidol effects in extreme conditions (experiments with animals)].

In extreme conditions like a new situation, bright light, open space, immobilization, height (the open field and lifted cruciform labyrinth test) and a conflict between an unavoidable action and fear of painful mexidol at the doses of 50 and 100 mg/kg of a body weight eliminates anxiety and fear in rats, recovers adequate reactions and the orientative-trying behavior, and lessens aggressiveness. Mexidol extends life span of mice in acute hypoxic conditions. Mexidol is highly competitive with diazepam as an anti-stress agent and excels it as an anti-hypoxic agent; in contrast to diazepam, mexidol does not cause sedation and myorelaxation.

Study of bipathic effect of phenazepam.

Phenazepam in ultralow doses significantly potentiated anxiolytic and anticonvulsant effects of therapeutic doses of the same drug both after preliminary or simultaneous administration, which attests to bipathic action of phenazepam. The combination of ultralow and therapeutic doses of phenazepam prevented the development of its specific myorelaxant and sedative side effects.

Involvement of the serotoninergic system in the mechanism of action of ultralow dose antibodies to S-100 protein.

The involvement of the serotoninergic system in the realization of anxiolytic and antidepressant activities of antibodies to S-100 protein in ultralow doses is proven. Administration of ultralow-dose antibodies to S-100 protein in combination with serotoninergic agents (ketanserin and 5-hydroxytryptophan) reduced the anxiolytic and antidepressant effects of antibodies.

[Combined action of mexidol and non-narcotic analgesics on pain thresholds and emotional stress behavior in animals].

The influence of non-narcotic analgesics analgin and pentalgin in the basic pharmacological effects of diazepam and mexidol has been studied in outbred male albino rats. It is established that both analgesics do not influence the activity of diazepam. At the same time, they potentiate the analgesic action of mexidol without influencing its antistress action and not inducing any side effects.

[Comparative study of the effects of amitriptyline, fluoxetine, and tianeptine on the amplitude of transcallosal evoked potentials].

The influence of amitriptyline, fluoxetine and tianeptine upon transcallosal responses has been studied in male albino rats. It is established that amitriptyline does not influence, fluoxetine reduces, and tianeptine increases the amplitude of evoked potentials. These data show evidence that tianeptine facilitates, fluoxetine impairs, and amitriptyline does not affect the interhemispheric transmission.

[Comparative study of the antidepressant and anxiolytic activity of fluoxetine and tianeptine].

The activity of fluoxetine (prozac) and tianeptine (coaxil) was studied in outbred male rats under Porsolt and S. Nomura modified forced swim tests. The antidepressant effect of tianeptine was much more pronounced that that of fluoxetine.

[Effect of typical and atypical anxiolytics on the behavior and electrophysiological parameters of rats with model cerebrovascular pathology].

The influence a series of anxiolytics (tranquilizers) on behavioral disturbances was studied in outbread white male rats with cerebrovascular pathology modeled by ligation of common carotid arteries. All studied anxiolytics (diazepam, buspirone, mexidol) exhibited more of less pronounced protective action with respect to the pathology studied. The most significant protective effect was produced by the atypical anxiolytic mexidol.

Design, synthesis, computational and biological evaluation of new anxiolytics.

New anxiolytics have been discovered by prediction of biological activity with computer programs pass and derek for a heterogeneous set of 5494 highly chemically diverse heterocyclic compounds (thiazoles, pyrazoles, isatins, a-fused imidazoles and others). The majority of tested compounds exhibit the predicted anxiolytic effect. The most potent activity was found in 2-(4-nitrophenyl)-3-(4-phenylpiperazinomethyl)imidazo[1,2-a]pyridine 8, 1-[(4-bromophenyl)-2-oxoethyl]-3-(1,3-dioxolano)-2-indolinone 3, 5-hydroxy-3-methoxycarbonyl-1-phenylpyrazole 5 and 2-(4-fluorophenyl)-3-(4-methylpiperazinomethyl)imidazo[1,2-a]pyridine 7.

[Stress-induced alteration of the antiaggressive effect of anxiolytics].

The influence of stresses of various etiology (prolonged isolation, inescapable electrostimulation) on the antiaggressive effect of anxiolytics was studied in outbread white male rats. It was established that, in contrast to the anticonflict effect (decreasing under the action of stress), then antiaggressive action of the drugs studied (diazepam, phenazepam, clonazepam, alprazolam) exhibits qualitative changes. In the absence of stress, the threshold of aggressive reaction is low and anxiolytics increase this level.

Design of new cognition enhancers: from computer prediction to synthesis and biological evaluation.

To discover new cognition enhancers, a set of virtually designed synthesizable compounds from different chemical series was investigated using two computer-aided approaches. One of the approaches is prediction of biological activity spectra for substances (PASS) and the second is prediction of toxicity, mutagenicity, and carcinogenicity (DEREK). To increase the probability of finding new chemical entities, we investigated a heterogeneous set of highly diverse chemicals including different types of heterocycles: five-membered (thiophenes, thiazoles, imidazoles, oxazoles, pyrroles), six-membered (pyridines, pyrimidines), seven-membered (diazepines, triazepines), fused five+six-membered heterocycles (indoles, benzothiazoles, purines, indolizines, neutral, mesoionic, and cationic azolopyridines).

GABAergic system in the anxiolytic effect of Proproten: experimental study.

The medicinal preparation Proproten contains ultralow doses of antibodies to S100 protein that acts as an important regulator of integrative activity in the brain and synaptic processes. Intracerebroventricular administration of Proproten, diazepam, and mexidol in doses of 2.5 ml/kg, 2 mg/kg, and 100 mg/kg, respectively, produced a strong anxiolytic effect on male outbred rats in the conflict situation and markedly increased the incidence of punished drinking.

Antidepressant properties of Proproten and amitriptyline: comparative experimental study.

Antidepressant properties of Proproten (antibodies to S100 protein in ultralow doses) were studied on outbred albino rats. The animals were subjected to the Porsolt's test of behavioral helplessness and Nomura's test of forced swimming in a reservoir with freely rotating wheels. Proproten in a dose of 2.