scholarly journals MECHANISMS OF ANALEPTIC AND ANTIGYPOXIC EFFECTS OF HETEROSIDES - DERIVATIVES OF SULFUR AND NITROGEN-CONTAINING HETEROCYCLES

2019 ◽  
pp. 46-53
Author(s):  
I. V. Kabachna ◽  
V. I. Kabachnyy ◽  
S. M. Drohovoz
Keyword(s):  
Theoretical Basis ◽  
Behavioral Responses ◽  
Antihypoxic Activity ◽  
Sodium Thiopental ◽  
Experimental Reproduction ◽  
The Awakening ◽  
Hypoxia With Hypercapnia ◽  
Derivatives Of ◽  
The Brain ◽  
Detoxification Mechanisms

In order to expand the theoretical basis of the purposeful search of analeptics, the awakening and antihypoxic properties of heteroside-21, heteroside-31 (derivatives of sulfur- and nitrogen-containing heterocycles) were studied and the mechanisms of their action were established. Sodium thiopental (42 mg/kg) was used to simulate suppression of the respiratory and vascular centers of the brain. The comparison drugs were – sulfocamphocaine (SCC) with combined analeptic action (20 mg/kg) and the antihypoxic drug piracetam (300 mg/kg). The results were obtained on the models of thiopental anesthesia and normobaric hypoxia with hypercapnia. The analysis of data allowed to count qualitatively and quantitatively the arousing and antihypoxic activity of new substances and classical drugs; their effect on the respiratory center of the brain and behavioral responses of animals; theoretically substantiate, experimentally confirm and establish aerobic, anaerobic and detoxification mechanisms of realization of effects in various conditions; to formulate the theoretical bases of purposeful search of universal analeptics and antihypoxic drugs and offer an instrumental-methodological complex for their experimental reproduction.

scholarly journals MECHANISMS OF ANALEPTIC AND ANTIGIPOXIC EFFECTS OF HETEROSIDES – (DERIVATIVES FOR SULFUR AND NITROGEN CONTAINING HETEROCYCLES)

World Science ◽  
2018 ◽  
Vol 1 (12(40)) ◽  
pp. 29-34
Author(s):  
Kabachna I. ◽  
Suprun E. ◽  
Kabachnyy V. ◽  
Serdiukova Yu.
Keyword(s):  
Behavioral Responses ◽  
Mechanisms Of Action ◽  
Antihypoxic Activity ◽  
Sodium Thiopental ◽  
The Awakening ◽  
Hypoxia With Hypercapnia ◽  
Derivatives Of ◽  
The Brain ◽  
Theoretical Foundations ◽  
Detoxification Mechanisms

In order to expand the theoretical base of targeted search for analeptics, the awakening and antihypoxic properties of Heterosides-21, Heterosides-31 (derivatives of sulfur and nitrogen containing heterocycles) were studied and their mechanisms of action were established. Sodium thiopental (42 mg/kg) was used to simulate suppression of the respiratory and vasomotor centers of the brain. Comparative drugs were the combined analeptic sulfocamphocaine (SCC) (20 mg/kg) and antihypoxant Piracetam (300 mg/kg).The results were obtained on the models of thiopental anesthesia and normobaric hypoxia with hypercapnia, the analysis of which allowed: to qualitatively and quantitatively assess the awakening, antihypoxic activity of the studied substances and classical preparations; their effect on the respiratory center of the brain and the behavioral responses of animals; theoretically substantiate, experimentally confirm and establish aerobic, anaerobic and detoxification mechanisms for the realization of effects in various conditions; to formulate the theoretical foundations of a targeted search for universal analeptics and antihypoxic drugs, to offer an instrumental and methodological complex for their experimental reproduction.

Evaluation of the activity of antihypoxants with an isothiourea structure in a model of hypercapnic hypoxia with a shutdown of the cerebral hemispheres

2021 ◽  
Vol 19 (1) ◽  
pp. 55-63
Author(s):  
Vera V. Marysheva ◽  
Vladimir V. Mikheev ◽  
Petr D. Shabanov
Keyword(s):  
Acute Hypoxia ◽  
Life Time ◽  
The Body ◽  
Cerebral Hemispheres ◽  
Antihypoxic Activity ◽  
Hypoxic Episode ◽  
Hypoxia With Hypercapnia ◽  
Hypercapnic Hypoxia ◽  
Outbred Mice ◽  
The Brain

PURPOSE: To study the effect of amtizol, 2-aminobenzthiazole (2-ABT) and 2-amino-4-acetylthiazolo[5,4-b]indole (BM-606) on the resistance of male outbred mice to acute hypoxia with hypercapnia under conditions of isolated functioning of one from the hemispheres, as well as both hemispheres of the brain. METHODS: A model of acute hypoxia with hypercapnia (canned hypoxia) was used in mice of the same mass, the lifespan of all animals was determined. Temporary shutdown of the cortex of one of the hemispheres or both hemispheres was achieved by epidural application of filter paper moistened with 25% potassium chloride solution, creating a spreading depression according to Leao. Amtizol, 2-aminobenzthiazole (2-ABT) and 2-amino-4-acetylthiazolo[5,4-b]indole (BM-606) at equimolar doses of 25, 32.5, and 50 mg/kg, respectively were used as pharmacological analyzers, the compounds were injected intraperitoneally 30 min before the hypoxic episode. RESULTS: It was shown that, in contrast to amtizol, 2-ABT and VM-606 increase the life time of experimental animals when any hemisphere is turned off. The use of drugs when both hemispheres were turned off revealed that amtizol has approximately equal effect on the brain and the rest of the body, in 2-ABT antihypoxic activity is 1/3 associated with the brain, in VM-606 exclusively with the brain. CONCLUSION: The experimental model used in this work makes it possible to quite easily evaluate the effect of either one drug or compare several drugs, their role in the functioning of the cerebral hemispheres, on which part of the sample highly resistant or low resistant to hypoxia they have the greatest effect.

EFFECT OF AMINOTHIOL ANTIHyPOXANTS ON INTERHEMISPHERIC ASyMMETRy OF THE bRAIN

2012 ◽  
Vol 10 (1) ◽  
pp. 51-53
Author(s):  
Vladimir Vladimirovich Mihkeev ◽  
Vera Vasilievna Marysheva ◽  
Boris Nikolaevich Bogomolov ◽  
Lubov Vladislavovna Zhukova-Williams
Keyword(s):  
Left Hemisphere ◽  
Right Hemisphere ◽  
Acute Hypoxia ◽  
Life Time ◽  
Antihypoxic Activity ◽  
Interhemispheric Relations ◽  
Hypoxia With Hypercapnia ◽  
Antihypoxic Effect ◽  
The Right ◽  
The Brain

The effect of aminothiol antihipoxants amthizol and its analogue VM-606 on the resistance of the SHR mice males to an acute hypoxia with hypercapnia under conditions of isolated functioning of one of the hemispheres of the brain was studied. Antihypoxic agent amthizol 25 mg/kg increases life time of naïve mice by 46.2%. The drug acted on the sham-operated mice more slightly, increasing of their life only on 28.1% (p<0.01). Administration of amthizol under conditions of functioning of the right hemisphere significantly enhanced (+64.8%) the life time of mice. No antihypoxic effect was registered after administration of amthizol to mice with active left hemisphere: the result was the same as in mice without amthizol. Therefore, antihypoxic effect of amthizol was due to its action on the right (but not the left) hemisphere of the brain. VM-606 possessed more antihypoxic activity in comparison with amthizol. After unilateral cortical inactivation, VM-606 increased life time of mice both in active right and active left hemispheres, but in more degree in active right hemisphere. Thus, interhemispheric differences in resistance of mice to hypoxia with hypercapnia were diminished. Therefore, the differences between amthizol and VM-606 are the followings: amthizol inverts interhemispheric relations in hypoxia whereas VM-606 diminishes them.

A Theoretical Basis for Emergent Pattern Discrimination in Neural Systems Through Slow Feature Extraction

2010 ◽  
Vol 22 (12) ◽  
pp. 2979-3035 ◽  
Author(s):  
Stefan Klampfl ◽  
Wolfgang Maass
Keyword(s):  
Feature Extraction ◽  
Theoretical Basis ◽  
Learning Algorithm ◽  
Temporal Cortex ◽  
Pattern Discrimination ◽  
Stimulus Onset ◽  
Inferior Temporal Cortex ◽  
Linear Discriminant ◽  
Discrimination Capability ◽  
The Brain

Neurons in the brain are able to detect and discriminate salient spatiotemporal patterns in the firing activity of presynaptic neurons. It is open how they can learn to achieve this, especially without the help of a supervisor. We show that a well-known unsupervised learning algorithm for linear neurons, slow feature analysis (SFA), is able to acquire the discrimination capability of one of the best algorithms for supervised linear discrimination learning, the Fisher linear discriminant (FLD), given suitable input statistics. We demonstrate the power of this principle by showing that it enables readout neurons from simulated cortical microcircuits to learn without any supervision to discriminate between spoken digits and to detect repeated firing patterns that are embedded into a stream of noise spike trains with the same firing statistics. Both these computer simulations and our theoretical analysis show that slow feature extraction enables neurons to extract and collect information that is spread out over a trajectory of firing states that lasts several hundred ms. In addition, it enables neurons to learn without supervision to keep track of time (relative to a stimulus onset, or the initiation of a motor response). Hence, these results elucidate how the brain could compute with trajectories of firing states rather than only with fixed point attractors. It also provides a theoretical basis for understanding recent experimental results on the emergence of view- and position-invariant classification of visual objects in inferior temporal cortex.

Difficulties with synaptic theory of learning and memory and possible remedies

2000 ◽  
Vol 23 (4) ◽  
pp. 550-551
Author(s):  
Mikhail N. Zhadin
Keyword(s):  
Cerebral Cortex ◽  
Associative Learning ◽  
Learning And Memory ◽  
Hebbian Learning ◽  
Behavioral Responses ◽  
Learning Rules ◽  
The Brain

The absence of a clear influence of an animal's behavioral responses to Hebbian associative learning in the cerebral cortex requires some changes in the Hebbian learning rules. The participation of the brain monoaminergic systems in Hebbian associative learning is considered.

scholarly journals Conversion of ethanolamine, monomethylethanolamine and dimethylethanolamine to choline-containing compounds by neurons in culture and by the rat brain

1989 ◽  
Vol 264 (2) ◽  
pp. 555-562 ◽  
Author(s):  
C Andriamampandry ◽  
L Freysz ◽  
J N Kanfer ◽  
H Dreyfus ◽  
R Massarelli
Keyword(s):  
Rat Brain ◽  
Primary Culture ◽  
De Novo ◽  
Water Soluble ◽  
Intraventricular Injection ◽  
Chick Embryos ◽  
Fetal Rat ◽  
Derivatives Of ◽  
The Brain

The incubation of neurons from chick embryos in primary culture with [3H]ethanolamine revealed the conversion of this base into monomethyl, dimethyl and choline derivatives, including the corresponding free bases. Labelling with [methyl-3H]monomethylethanolamine and [methyl-3H]dimethylethanolamine supported the conclusion that in chick neuron cultures, phosphoethanolamine appears to be the preferential substrate for methylation, rather than ethanolamine or phosphatidylethanolamine. The methylation of the latter two compounds, in particular that of phosphatidylethanolamine, was seemingly stopped at the level of their monomethyl derivatives. Fetal rat neurons in primary culture incubated with [3H]ethanolamine showed similar results to those observed with chick neurones. However, phosphoethanolamine and phosphatidylethanolamine and, to a lesser extent, free ethanolamine, appeared to be possible substrates for methylation reactions. The methylation of water-soluble ethanolamine compounds de novo was further confirmed by experiments performed in vivo by intraventricular injection of [3H]ethanolamine. Phosphocholine and the monomethyl and dimethyl derivatives of ethanolamine were detected in the brain 15 min after injection.

Central monoaminergic systems sensitivity to acute hypoxia with hypercapnia changes after the maintenance under the long-term social isolation

2018 ◽  
Vol 64 (6) ◽  
pp. 511-516 ◽  
Author(s):  
I.V. Karpova ◽  
V.V. Mikheev ◽  
V.V. Marysheva ◽  
N.A. Kuritcyna ◽  
E.R. Bychkov ◽  
...  
Keyword(s):  
Cerebral Cortex ◽  
Social Isolation ◽  
Acute Hypoxia ◽  
Brain Structures ◽  
Hypoxia With Hypercapnia ◽  
Long Time ◽  
The Right ◽  
The Brain ◽  
Monoamines And Their Metabolites

The experiments were performed in male albino outbred mice kept in a group and under the conditions of long-term social isolation. The changes in the monoaminergic systems of the left and right hemispheres of the brain after acute hypoxia with hypercapnia have been studied. The levels of dopamine (DA), serotonin (5-HT) and their metabolites – dioxyphenylacetic (DOPAC), homovanillic (HVA), and 5-hydroxyindoleacetic (5-HIAA) acids – were determined by HPLC in the cerebral cortex, hippocampus and striatum of the right and left sides of the brain. In the control mice kept both in the group and under the conditions of social isolation, a higher content of DA in the cortex of the left hemisphere has been found. In the other brain structures the monoamine content was symmetric. In the cerebral cortex of the mice in the group, acute hypoxia with hypercapnia led to a right-sided increase in the DA and 5HT levels. At the same time, the DOPAC content decreased in the left cortex. In mice in the group, under the hypoxia with hypercapnia conditions, the DA level in the left hippocampus increased. In the striatum, the content of monoamines and their metabolites did not change significantly. In animals kept for a long time under the conditions of social isolation, hypoxia with hypercapnia no statistically significant changes in the monoamines and their metabolites levels were found. It has been concluded that the preliminary maintenance under the conditions of prolonged social isolation changes the reaction of central monoaminergic systems to acute hypoxia with hypercapnia.

scholarly journals Inconsistencies in the assessment of food intake

2012 ◽  
Vol 303 (12) ◽  
pp. E1408-E1418 ◽  
Author(s):  
Stephen C. Woods ◽  
Wolfgang Langhans
Keyword(s):  
Food Intake ◽  
Energy Intake ◽  
Body Fat ◽  
Energy Homeostasis ◽  
Behavioral Responses ◽  
Normal Function ◽  
Direct Proportion ◽  
Heated Debate ◽  
The Brain ◽  
Reducing Energy

Many peptides and other compounds that influence metabolism also influence food intake, and numerous hypotheses explaining the observed effects in terms of energy homeostasis have been suggested over the years. For example, cholecystokinin (CCK), a duodenal peptide secreted during meals that aids in digestion, also reduces ongoing food intake, thereby contributing to satiation; and insulin and leptin, hormones secreted in direct proportion to body fat, act in the brain to help control adiposity by reducing energy intake. These behavioral actions are often considered to be hard-wired, such that negative experiments, in which an administered compound fails to have its purported effect, are generally disregarded. In point of fact, failures to replicate the effects of compounds on food intake are commonplace, and this occurs both between and within laboratories. Failures to replicate have historically fueled heated debate about the efficacy and/or normal function of one or another compound, leading to confusion and ambiguity in the literature. We review these phenomena and their implications and argue that, rather than eliciting hard-wired behavioral responses in the maintenance of homeostasis, compounds that alter food intake are subjected to numerous influences that can render them completely ineffective at times and that a major reason for this variance is that food intake is not under stringent homeostatic control.

Differential electrophysiological and behavioral responses to optically active derivatives of phencyclidine

1981 ◽  
Vol 315 (3) ◽  
pp. 203-209 ◽  
Author(s):  
Jwaharlal Marwaha ◽  
Michael Palmer ◽  
Barry Hoffer ◽  
Robert Freedman ◽  
Kenner C. Rice ◽  
...  
Keyword(s):  
Behavioral Responses ◽  
Optically Active ◽  
Derivatives Of
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