RESUMEN

It has been shown in experiments on anesthetized cats and dogs that lithium hydroxybutyrate produces antiarrhythmic action in central aconitic and strophanthine arrhythmias, prevents the development of ventricular fibrillation, and shows antiarrhythmic activity in strong occlusion on the coronary artery. The drug does not remove the atrial and aconitic patterns of arrhythmia. Lithium chloride also exhibits antiarrhythmic action in central aconitic arrhythmia, being inferior to lithium hydroxybutyrate. The drug does not influence central strophanthine arrhythmia and does not show antifibrillation activity.

Asunto(s)

RESUMEN

It has been shown in experiments on guinea-pigs sensitized with ragweed pollen (Ambrosia artemisiifolia) that dimebon (9-/2-(2-methylpyridyl-5) ethyl/3,6- dimethyl-1, 2, 3, 4-tetrahydro-gamma-carboline dihydrochloride), a new antihistaminic drug, exerts a marked antianaphylactic effect which compares very favourably with that of phencarol. When administered in the minimal effective doses, dimebon is less active than ketotifen, whereas in doses of 2.5 and 5 mg/kg it, is more effective. Marked anaphylactic activity of the drug is accounted for by its antihistaminic and antiserotonin actions. When administered intragastrically, subcutaneously and intravenously, dimebon is less toxic than phencarol (by 1.28, 1.78 and 1.43 times, respectively) and ketotifen (by 1.78, 1.68 and 5 times, respectively).

Asunto(s)

RESUMEN

Hexahydroubiquinone-4 (H6CoQ4) and ubiquinone-9 (CoQ9) in the form of solutions in vegetable oil administered to mice and rats subcutaneously and intragastrically produced a radioprotective effect comparable with that of cystamine. Under the accepted experimental conditions the compounds did not produce any therapeutic effect.

Asunto(s)

RESUMEN

It has been shown in experiments on Wistar rats and random-bred mice that dimebon does not accelerate burn wound healing but has a protective action when applied intraperitoneally and intragastrically, thereby raising the animals' survival rate in burn shock.

Asunto(s)

Asunto(s)

Asunto(s)

RESUMEN

Experiments were made on random-bred and linear mice, Wistar rats, rabbits and dogs to examine pharmacological properties of ubiquinone-9 and hexahydroubiquinone-4. Both compounds (oily solutions) administered intraperitoneally, intragastrically and subcutaneously in single and multiple doses produced no changes in the behavior or status of the animals, which might have attested to their toxicity. They were found to exert a regulatory action on the central nervous system, decreasing its sensitivity to numerous narcotic and convulsant substances without appreciable effects on the blood, arterial pressure, ECG and diuresis. The main obstacle for comprehensive experimental study and application of these substances in medical practice lies in the absence of a perfect medicinal form.

Asunto(s)

Asunto(s)

RESUMEN

Compounds that possess long-term anesthetic effect have been found among phenylethylamine derivatives substituted by O-alkyl (position 4) or O-benzyl (positions 2, 3 and 4) radicals. It was shown that these compounds compare very favourably with novocain, since their anesthetic effect exceeds 54.8 - 66.9-fold that produced by novocain. Such an effect is a consequence of neurolytic properties of the compounds synthesized.

Asunto(s)

RESUMEN

Toxicity and radioprotective properties of 17 chemical compounds containing a hydrazine fragment have been studied in experiments on mice. It has been established that the radioprotective action of the test compounds does not depend substantially on whether the hydrazine fragment enters the heterocyclic moiety fully, partly or as an exocyclic substituent in the ring.

Asunto(s)

RESUMEN

It was reported previously that the analogues of dimecabin (1,2-dimethyl-3-carbethoxy-5-oxyindole),2-methyl-3-carbethoxy-5-oxyindole and the derivatives of 2-methyl-3-carbethoxy-4, 5, 6, 7-tetrahydroindole substituted in the 1st position reduce the content of argentaffinic substance in enterochromaffin cells (EC) for a long period of time. It has been shown that "recognizability" of the acetyl derivatives of 4, 5, 6, 7-tetrahydroindole by the EC receptor systems is preserved. Administration of the acetyl derivatives into the stomach (10 mg/kg for 5 days) induce a prolonged decrease in the argentaffin substance content in EC, and augment the noradrenaline level without exerting a pronounced effect on the dopamine content. These substances also inhibit monoamine oxidase and acetylcholinesterase activity in the rat brain. Detection in EC of the biologically active substances common to the APUD-system and the brain suggests a new trend in the study into the action mode of indole compounds.

Asunto(s)

RESUMEN

Acute toxicity and radioprotective properties of 16 derivatives of tetrahydro- and dihydropyrimidines were studied in experiments on mice. Hydroiodides of 4,6,6-trimethyl-3,R-2-methylthio-3,6-dihydropyrimidines were shown to be more toxic than respective hydroiodides of 4,6,6-trimethyl-3-R-2-methylthio-4-oxy-3,4,5,6-tetrahydropyrimidines. Four compounds exhibited moderate radioprotective properties.

Asunto(s)

RESUMEN

Toxicity and radioprotective properties of 18 derivatives of oxazine and thiazine with a varying degree of the cycle saturation were studied in experiments on mice. Monotypic regularity in variations of their toxic properties relative to the chemical structure was noted. 4,4,6-Trimethyl-2-dimethylamino-4H-1,3-oxazine exerted a pronounced radioprotective action.

Asunto(s)

RESUMEN

Toxicity, radioprotective and antiinflammatory properties of 20 vinyl derivatives of quinoline and products of their transformations were studied in experiments on Wistar mice and rats. The salts of quinoline vinyl derivatives (compounds VI, IX, XII, and XVIII) were shown to be more toxic than respective initial compounds (VI, VIII, XI and XVI). 8-(beta-Butylthio)-ethyloxyquinoline (compound IV) protected 25% of irradiated mice from death. Compounds I, XII, XVI and XVIII exerted a radioprotective action (in 10-15%), whereas the remaining substances proved ineffective. The combination of 8-vinyloxyquinoline and iodine (compound IV) elicited a marked antiinflammatory action in experimental serotonin-, dextran- and to a less measure formalin-induced inflammation.

Asunto(s)

RESUMEN

Test on mice demonstrated the radio-protective activity of 12 derivatives of 4-oxyhexahydropyrimidinethione-2 and 1,2,3,6-tetrahydropyrimidinethione-2 well-marked with intraperitoneal administration 10--20 minutes prior to irradiation (1000 r, exposure dose rate--10 r/min). As a whole the tetrahydroderivates are more toxic.

Asunto(s)

RESUMEN

The toxicity of radioprotective and some pharmacological properties of 33 compounds, phenylethylamine derivatives, substituted in the phenyl ring were studied. Some of these display radioprotective and curative properties and also produce anesthetizing, coronary dilating, antiarrhythmic and other effects.

Asunto(s)

RESUMEN

Test set up on albino rats demonstrated a preliminary introduction of amichlophene to prevent a hypoxic fall in the level of highly ergastic compounds in the tissues owing to stimulation of the mitochondrial respiration processes and increased energy-producting effectiveness of the latter. The beneficial effect of amichlophen on the bioenergetics of the tissues in acute hypoxia is largely caused by the continued structural and functional integrity of the mitochondria, lysosomes and other cellular organellae which is due to the inhibitory action of the compound on the prosses of lipids reoxidation and to the activity of phospholipase A.

Asunto(s)

RESUMEN

Among some derivatives of p-chlorophenoxyacetic acid (dialkylaminoethyl, diethylaminoethylmercaptomercaptan and tropine ethers, dialkylaminoethylene amides) there have been discovered compounds with marked neurotropic, locally anesthetic, antiarrhythmic and antihypoxic properties.

Asunto(s)

Asunto(s)

Asunto(s)