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12 results on '"Kliuntina TV"'

1. Norbornan, a new irreversible ligand of the GABAA-receptor chloride channels

Author

A. I. Golovko, G. A. Sofronov, and Kliuntina Tv

Subjects
Chemistry, GABAA receptor, Ionophore, General Medicine, Ligand (biochemistry), General Biochemistry, Genetics and Molecular Biology, Acylation, chemistry.chemical_compound, Membrane, Biophysics, Convulsant, Chloride channel, Organic chemistry, Norbornane
Abstract

In vitro experiments demonstrate the high affinity of the toxic convulsant norbornan [2,2-di-(trifluoromethyl)-3,3-dicyano-5,6-dichloronorbornane] for the GABAA-receptor chloride channels of membranes from rat brain. Repeated washing and centrifugation do not restore the ionophore density on norbornan-treated membranes, suggesting that norbornan may be counted among the agents acylating the chloride channels.

Published
1996
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2. [Formation of elevated sensitivity to seizures induced by a single administration of norbornan].

Author

Golovko AI, Ivanov MB, Kliuntina TV, Sofronov GA, Sviderskiĭ OA, and Shilov VV

Subjects
3-Mercaptopropionic Acid metabolism, 3-Mercaptopropionic Acid toxicity, Animals, Chloride Channels antagonists & inhibitors, Convulsants metabolism, GABA-A Receptor Antagonists, Lethal Dose 50, Male, Mice, Norbornanes metabolism, Picrotoxin metabolism, Picrotoxin toxicity, Synaptic Membranes drug effects, Synaptic Membranes metabolism, Convulsants toxicity, Kindling, Neurologic drug effects, Norbornanes toxicity
Published
1997

3. [The effect of perftoran on the resistance of mice to GABA receptor antagonists and on the antidote activity of anticonvulsant agents].

Author

Golovko AI, Kliuntina TV, Ivanov MB, Sofronov GA, Sviderskiĭ OA, and Shilov VV

Subjects
Animals, Bicuculline poisoning, Diazepam therapeutic use, Drug Evaluation, Preclinical, Drug Resistance, Drug Synergism, Fluorocarbons pharmacology, Male, Mice, Phenobarbital therapeutic use, Picrotoxin poisoning, Poisoning drug therapy, Receptors, GABA-A drug effects, Receptors, Muscarinic drug effects, Anticonvulsants therapeutic use, Antidotes therapeutic use, Fluorocarbons therapeutic use, GABA Antagonists poisoning
Abstract

Perfluorane (a phenobarbital-type inducer of the microsomal enzyme system) raised the resistance of mice to the toxic effect of picrotoxin and bicucullin in 7 days after injection. The antidote effect of diazepam and phenobarbital increased under such conditions. In experiments in vitro a modulatory effect of perftorane on the central muscarine and benzodiazepine receptors was demonstrated.

Published
1996

4. [Changes in the density of GABAA receptor chloride channels in rodent brain induced by norbornane].

Author

Golovko AI, Sofronov GA, Kliuntina TV, Suftin SG, and Garbuz LA

Subjects
Acylation, Animals, Brain metabolism, Bridged-Ring Compounds pharmacology, Chloride Channels metabolism, Convulsants metabolism, GABA Antagonists pharmacology, Ligands, Male, Mice, Norbornanes metabolism, Rats, Receptors, GABA-A metabolism, Seizures chemically induced, Synaptic Membranes drug effects, Synaptic Membranes metabolism, Brain drug effects, Chloride Channels antagonists & inhibitors, Convulsants pharmacology, GABA-A Receptor Antagonists, Norbornanes pharmacology
Published
1996

5. [Norbornane--a new irreversible ligand of the GABA-A receptor chloride channels].

Author

Golovko AI, Sofronov GA, and Kliuntina TV

Subjects
Acylation, Animals, Binding Sites, Brain drug effects, Brain metabolism, Chloride Channels metabolism, Ionophores metabolism, Ligands, Male, Norbornanes metabolism, Rats, Receptors, GABA-A metabolism, Chloride Channels drug effects, Norbornanes pharmacology, Receptors, GABA-A drug effects
Published
1996

6. [The effect of salicylates on the toxicity of GABAlytics for mice].

Author

Golovko AI, Sofronov GA, and Kliuntina TV

Subjects
Animals, Drug Interactions, Male, Mice, Protein Synthesis Inhibitors pharmacology, Receptors, GABA-A drug effects, Salicylic Acid, Serum Albumin biosynthesis, Serum Albumin metabolism, Aspirin pharmacology, Bicuculline toxicity, GABA Antagonists toxicity, Picrotoxin toxicity, Salicylates pharmacology
Published
1995

7. [The effect of paraoxon and sulfhydryl reagents on the binding of 3H-quinuclidinyl benzilate and 3H-methylscopolamine with synaptic membranes of rat cerebral cortex].

Author

Golovko AI, Sofronov GA, Kurganova TA, and Kliuntina TV

Subjects
Animals, Binding Sites, Cerebral Cortex metabolism, Male, N-Methylscopolamine, Rats, Receptors, Cholinergic metabolism, Synaptic Membranes metabolism, Tritium, Cerebral Cortex drug effects, Paraoxon pharmacology, Quinuclidinyl Benzilate metabolism, Scopolamine Derivatives metabolism, Sulfhydryl Reagents pharmacology, Synaptic Membranes drug effects
Published
1994

9. [The effect of 3-mercaptopropionic acid on the toxicity of GABA-lytics for mice].

Author

Golovko AI, Sofronov GA, and Kliuntina TV

Subjects
Animals, Brain drug effects, Brain metabolism, Bridged Bicyclo Compounds metabolism, Drug Synergism, Ligands, Male, Mice, Synaptic Membranes drug effects, Synaptic Membranes metabolism, Time Factors, gamma-Aminobutyric Acid metabolism, 3-Mercaptopropionic Acid pharmacology, Bicuculline toxicity, Bridged Bicyclo Compounds, Heterocyclic, GABA Antagonists, Picrotoxin toxicity, gamma-Aminobutyric Acid drug effects
Abstract

The influence of 3-mercaptopropionic acid (3-MPA) on toxicities of bicuculline and picrotoxin was evaluated in mice. It was demonstrated that 3-MPA pretreatment for 5 min increased the toxicities of bicuculline and picrotoxin by 26% and 31%, respectively. 3-MPA did not alter the binding of (3H)TBOB and (3H)GABA to synaptosomal brain membranes of intact mice. The changes in toxicity may be associated with increased binding of GABA-antagonists to their receptors due to decreased brain GABA.

Published
1993

10. [The effect of triorthocresyl phosphate on the toxicity of GABA-lytics for mice].

Author

Golovko AI, Sofronov GA, Nikolaeva TV, Pluzhnikov NN, and Kliuntina TV

Subjects
3-Mercaptopropionic Acid toxicity, Animals, Bicuculline toxicity, Brain drug effects, Brain metabolism, Bridged Bicyclo Compounds metabolism, Carboxylic Ester Hydrolases blood, Carboxylic Ester Hydrolases drug effects, Drug Interactions, In Vitro Techniques, Ligands, Male, Mice, Picrotoxin toxicity, Synaptic Membranes drug effects, Synaptic Membranes metabolism, gamma-Aminobutyric Acid metabolism, Bridged Bicyclo Compounds, Heterocyclic, GABA Antagonists, Tritolyl Phosphates pharmacology, gamma-Aminobutyric Acid drug effects
Abstract

The toxicity of the picrotoxin bicuculline, but not of 3-mercaptopropionic acid increased in mice pretreated with triorthocresyl phosphate (TOCP). TOCP decreased the affinity of brain GABA receptors of intact mice for [3H] GABA. The binding of [3H]-t-butylcycloorthobenzoate was unchanged. The increased toxicity of GABA-antagonists may be associated with inhibition of blood carboxylesterases. The possibility of direct influence of TOCP and its metabolites on the GABA/benzodiazepine receptor complex cannot be excluded.

Published
1993

11. [N-methyl-3H]methylphenazepam--a new ligand for benzodiazepine receptors].

Author

Golovko AI, Sofronov GA, and Kliuntina TV

Subjects
Animals, Corpus Striatum ultrastructure, Diazepam metabolism, Male, Muscimol metabolism, Radioligand Assay, Rats, Tritium, gamma-Aminobutyric Acid metabolism, Anti-Anxiety Agents, Benzodiazepines, Benzodiazepinones metabolism, Corpus Striatum metabolism, Receptors, GABA-A metabolism, Synaptic Membranes metabolism
Abstract

The binding of [N-methyl-3H] methylphenazepam with synaptosomal membranes of rat striatum was studied. The affinity of binding sites to this ligand was higher when compared with [3H] diazepam. No changes in maximal binding capacity were found in two groups. GABA and muscimol increased the binding of [3H] diazepam and had no effect on binding of [N-methyl-3H] methylphenazepam. Diazepam and phenazepam competitively decreased the [N-methyl-3H] methylphenazepam binding. The inhibitor activity of phenazepam was higher.

Published
1993

12. [Effects of diisopropylfluorophosphate, paraoxon and dichlophos on [3H] quinuclidinyl benzylate binding to the rat striatum synaptic membranes].

Author

Golovko AI, Sofronov GA, Nikolaeva TV, and Kliuntina TV

Subjects
Animals, Corpus Striatum drug effects, In Vitro Techniques, Male, Rats, Receptors, Muscarinic drug effects, Seizures metabolism, Synaptosomes drug effects, Corpus Striatum metabolism, Dichlorvos pharmacology, Isoflurophate pharmacology, Paraoxon pharmacology, Quinuclidinyl Benzilate metabolism, Synaptosomes metabolism
Abstract

The binding of [3H] quinuclidinyl benzilate (QNB) to rat striatum membranes after diisopropylfluorophosphate (DFP) induced seizures was characterized. There was a 36% decrease in Kd and a 33% decrease in the number of muscarinic receptors. Paraoxon caused inhibition fo [3H] QNB binding to the striatal membranes of intact rats. It is possible that a direct action of DFP on the muscarinic receptor is not the cause of anti-cholinesterase-induced changes in [3H] QNB binding.

Published
1992

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