ABSTRACT
Four new derivatives of glutamic and gamma-aminobutyric acids influencing the central nervous system were produced. By the character of their action they refer to the substances of the sedating tranquilizing type without the myorelaxant component. The drug activity degree depends on its ability to penetrate through cell membranes that is in turn determined by the structure of the compound.
Subject(s)
Glutamates/pharmacology , Nicotinic Acids/pharmacology , Psychotropic Drugs/pharmacology , gamma-Aminobutyric Acid/analogs & derivatives , Animals , Cell Membrane Permeability/drug effects , Dose-Response Relationship, Drug , Glutamic Acid , Mice , Motor Activity/drug effects , Structure-Activity Relationship , gamma-Aminobutyric Acid/pharmacologyABSTRACT
Experiments on 75 dogs with experimental myocardial infarction were made to study and compare the therapeutic effect of nicamag (a mixture of potassium and magnesium nicotinates) in a dose of 10 mg/kg, panangin and asparkam (potassium and magnesium aspartates). Nicamag rapidly precipitated postinfarction arrhythmia and made the ECG completely return to normal in the majority of cases. A beneficial effect of the drug on carbohydrate, energy and electrolyte metabolism in the myocardium was discovered to underlie the above-described action. Nicamag abruptly lowered the titers of cardial antibodies, increased the fibrinalytic activity of the blood which is accounted for by the effect of the anion--nicotinic acid.
Subject(s)
Aspartic Acid/analogs & derivatives , Myocardial Infarction/drug therapy , Potassium Magnesium Aspartate/analogs & derivatives , Potassium Magnesium Aspartate/therapeutic use , Vasodilator Agents/therapeutic use , Adenosine Triphosphatases/metabolism , Adenosine Triphosphate/metabolism , Animals , Dogs , Drug Combinations , Energy Metabolism , Lactates/metabolism , Lactic Acid , Myocardium/metabolism , Pyruvates/metabolism , Pyruvic AcidABSTRACT
It has been shown in rat experimental aconitinic arrhythmia and in dog postinfarction arrhythmia that combined potassium and magnesium nicotinates show a pronounced anti-arrhythmic effect. The studies on the drug distribution in the tissues indicate that the content of potassium, magnesium and total coenzymatic forms of nicotinic acid rises in the myocardium by the 12th hour from the commencement of the drug administration. Intracellular and exocellular content of potassium and sodium has been shown to return to normal.
