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1.
Farmakol Toksikol ; 42(1): 7-11, 1979.
Article in Russian | MEDLINE | ID: mdl-217728

ABSTRACT

Levomepromazine, chlorpromazine (10 and 30 mg/kg), etaperaxine, haloperidol (3 and 10 mg/kg) inhibited the exploratory-motor reactions of rats and the brain Na, K-ATPase activity an hour after their administration. The effects of tranquilizers as well as of antidepressants on the exploratory reactions and on the enzyme activity were not found to stand in a clearcut relation to each other. The stimulating effect of amphethamine (3 mg/kg) was accompanied by activation and suppressive action (10 mg/kg)--by inhibition of the enzyme. It is suggested that the inhibition of the brain Na, K-ATPase activity by psychotropic drugs may play a role in the mechanism of their sedative action.


Subject(s)
Brain/drug effects , Exploratory Behavior/drug effects , Psychotropic Drugs/pharmacology , Sodium-Potassium-Exchanging ATPase/metabolism , Amphetamine/pharmacology , Animals , Benactyzine/pharmacology , Chlorpromazine/pharmacology , Diazepam/pharmacology , Haloperidol/pharmacology , Imipramine/pharmacology , Iproniazid/pharmacology , Male , Methotrimeprazine/pharmacology , Perphenazine/pharmacology , Rats , Trazodone/pharmacology
2.
Ukr Biokhim Zh ; 48(3): 326-31, 1976.
Article in Russian | MEDLINE | ID: mdl-134479

ABSTRACT

The activity of Na+, K+-ATPase from bovine brain in vitro was studied as affected by some neuroleptics (levomepromazine, chlorpromazine, perphenazine and haloperidol), antidepressants (imipramine and iproniazid) and psychostimulants (amphetamine) as well as by benactyzine and procaine. The degree of the enzyme inhibition by these drugs estimated by means of I 50 and apparent inhibitor constants (Ki) or rate constants (k) was different. Sensitivity of the brain Na+, K+-ATPase to the drugs decreased in the following order: levomepromazine, chlorpromazine, perphenazine, haloperidol, imipramine, iproniazid, benactyzine, procaine and amphetamine. Competition for the enzyme was revealed between sodium and some of the drugs investigated (levomepromazine, chlorpromazine, perphenazine and impramine) as well as between potassium and other drugs (haloperidol, genactyzine and amphetamine). It is suggested that the inhibition of the brain Na+, K+-ATPase by psychotropic drugs may be a part in the biochemical mechanism of their sedative-tranquilizing activity.


Subject(s)
Adenosine Triphosphatases/metabolism , Brain/enzymology , Psychotropic Drugs/pharmacology , Adenosine Triphosphatases/antagonists & inhibitors , Amphetamine/pharmacology , Animals , Benactyzine/pharmacology , Brain/drug effects , Cattle , Chlorpromazine/pharmacology , Enzyme Activation/drug effects , Enzyme Repression/drug effects , Haloperidol/pharmacology , Imipramine/pharmacology , In Vitro Techniques , Iproniazid/pharmacology , Methotrimeprazine/pharmacology , Perphenazine/pharmacology , Potassium/metabolism , Procaine/pharmacology , Sodium/metabolism
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