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At least 19 recordsLinked to original sources
PubMed1975

[Elektrophysiological parameters of mollusk neurons under the influence of etimizol].

Extracellular application of 5--10 mM/L etimizol exerted a specific effect on the giant neurons of the Coretus corneus isolated nervous system: action potential duration increased significantly, speed of development of its descending phase decreased, as well as the trace hyperpolarization amplitude. The effect was reversible and depended upon the etimizol concentration and the initial functional state of neurons. Etimizol is supposed to decrease the K-+ permeability of neurons' membrane during action potential. Large concentrations of etimizol decrease, probably, the Na+ permeability as well as suggested by reducing maximum of the ascending phase of action potential.

Action Potentials↗
PubMed1990

[Vasodilating effects of etimizol in vitro and its relation to purinergic receptors].

The paper is concerned with the effect of the breath analeptic agent etimizole on the smooth muscle of vessels under in vitro conditions from the viewpoint of its assumed interaction with purinergic receptors. Isolated preparations of the coronary artery and a. dorsalis pedis of the dog served as experimental material. Etimizole administered in a cumulative manner in dependence on concentration decreases the strength of contraction of the preparations contracted with K+ ions. This relaxant effect, similarly as the effect of adenosine, is not affected by a removal of the endothelium, can be inhibited with theophylline and potentiated with dipyridamole. Etimizole in higher concentrations inhibits the response of vascular preparations to electrical stimulation. In the concentration of 10(-4) mol.l-1 it potentiates the relaxant effect of adenosine, the experimental effects not differing from the theoretical curve for the addition of effects. The obtained results support the assumption that the vasodilating effect of etimizole is mediated prevalently by P1 purinergic receptors.

Adenosine↗
PubMed1986

[Etimizol absorption from the small intestine in dogs: the dependence on dosage].

As etimizol has been previously reported to be of low bioavailability, the kinetics of its absorption from the dog intestinal loop was investigated in chronic experiments. After administration of etimizol at doses of 10 or 1 mg/loop mean residence time of etimizol in the loop was 20.1 and 7.6 min, respectively, with mean standard deviation being 3.1 and 0.8, respectively. It was concluded that overall etimizol absorption from small intestine was high and its low bioavailability resulted from presystemic drug metabolism, as well as that the absorption kinetics was dose-dependent, with saturation reached at higher drug doses.

Animals↗
PubMed1985

[Effect of etimizol on instrumental learning in rats].

The action of etimizol on the acquisition of the conditioned reflexes with different complexity and biological significance of reinforcement was studied. The acquisition was performed in a shuttle box and U-shaped maze using food and footshock stimuli. The time interval between administration of etimizol (3 mg/kg) and the onset of learning varied between 0.5 and 3 h in the several series. Etimizol did not facilitate the learning in rats whatever the time of administration and biological modality of reinforcement. It is suggested that the positive effect of etimizol on the memory is related to its influence on the consolidation stage.

Animals↗
PubMedDate not supplied

[The significance of the antihypoxic properties of etimizol in its nootropic action].

The antihypoxic effects of etimizol and other nootropics are analysed on various experimental models of hypoxia and during bicycle ergometric exercise in healthy volunteers. Etimizol was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain). The advantage of etimizol as compared to other nootropics with similar action (meclofenoxate, piracetam) is its high effectiveness at a single administration.

Amnesia↗
PubMed1988

[Use of biological methods in the analysis of the purinergic activity of etimizol].

To analyse etimizol purinergic activity, methods of biological analysis were applied using isolated smooth muscle strips of the guinea-pig caecum and developing embryo cultures of the sea urchin (Strongylocentrotus intermedius). Stimulating etimizol action in 10(-8)-10(-12) M concentration was observed on embryonal development in the sea urchin to be eliminated by co-action of etimizol and P1-purinoceptor antagonist theophylline. The analogous action of the preparations was established using isolated smooth muscle strips of the guinea-pig caecum.

Animals↗
PubMed1983

[Dynamics of the distribution of labeled etimizol in brain cell structures].

The time course of 14C-etimizol distribution in cell structures of the rat cerebral cortex was studied. Two minutes after intraperitoneal injection etimizol penetrates brain cells. At this time the greater portion of the drug is found in cytosol. In five minutes the maximal part of the label gets bound with cell nuclei and microsomal protein fraction extracted with 0.14 M NaCl. These two cell fractions show the highest radioactivity throughout the entire observation period (up to 7 days). Since these fractions are reported to be capable of calcium accumulation, a suggestion is made that metabolic effects of etimizol are likely to be related to calcium metabolism.

Animals↗
PubMed1989

[Role of sex dimorphism in the pharmacological action of etimizol].

It has been shown that in female rats the level of ACTH, corticosterone in the blood, relative mass of adrenals, maintenance of T3, T4 in the serum and liver was significantly higher, but the activity of liver enzyme microsomes system was lower than in males; no sex differences were observed in myocardial creatine phosphokinase system. The influence of the etimizol on the female rats significantly speed up amidopyrine N-demethylation and biotransformation of hexobarbital. In males these systems react less on etimizol, but it reduces the speed of amidopyrine N-demethylation.

Adrenal Glands↗
PubMedDate not supplied

[Molecular bases for the action of etimizol].

Experiments on rats were made to study the molecular mechanism of the action of a new original neurotropic drug etimizol administered in a dose of 10-25 mg/kg. It was shown that it activates brain cAMP, increases the concentration of Ca2+ and membrane permeability of brain synaptosomes. The drug was also shown to enhance genome activity of the brain cells and to intensity energy metabolism. It is concluded that the molecular mechanism of etimizol action is related to the activation of the adenyl cyclase system and to the increased cAMP content, thereby leading to the activation of gene transcription, intensification of metabolic processes, and to the increased synaptic conduction.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed2002

[Different therapeutic approaches for chronic diffuse liver lesions using ornicetil, lactulose, etimizol and corinfar].

Different therapeutic regimens were tried in 67 patients with hepatic cirrhosis and in 54 patients with chronic hepatitis depending on the leading pathological syndrome. Treatment schemes involved the use of the drug ornicetil in patients having acute episodes of portal systemic encephalopacy, lactulose in those presenting with an increased content of ammonia in the blood and symptoms of chronic portal systemic encephalopacy; etimizol was given to those patients with an apperant antioxidant imbalance. Differentiated approaches to the institution of curative measures permitted improving considerably the patients' medical rehabilitation, achieving regression of pathological manifestations. It has been found out that the above drugs exert a positive effect on the cytolytic and mesenchimal-inflammatory syndromes and will, we believe, come to be widely used for treating diffuse lesions of the liver.

Etimizol↗
PubMedDate not supplied

[Analysis of the hypothermic action of etimizol].

In chronic experiments on rabbits it was shown that the hypothermic effect appears in the series of antipheins after the addition of ethyl radical in the first position of imidazole ring. The hypothermic effect of etimizol is more pronounced in the brain than in the body, whereas caffeine equally increases the temperature of the brain and body.

Animals↗
PubMedDate not supplied

[Prophylactic and therapeutic action of etimizol on the change in myocardial tissue metabolism in a neurogenic lesion].

The effect of aethimizol, introduced to rabbits before and after inflicting a 3-hours long extraordinary stimulation applied to the reflexogenic zone of the aortic arch, was studied. Investigations covered some aspects of energy metabolism and the level of the norepinephrine mediator in the muscle of the heart and also the functional state of the latter. Aethimizol was found to prevent shifts of the studied metabolic factors, induced by electric stimulation, and also to avert depletion of norepinephrine in the tissue of the myocardium and normalize its function.

Animals↗
PubMedDate not supplied

[The effect of etimizol on the excitability and spontaneous super-slow activity of the structures of the rabbit brain].

Spontaneous superslow electrical brain activity and its changes were studied in acute experiments on curarized rabbits after administration of etimysol in doses of 1.0, 1.5 and 2.5 mg/kg. The effect of the drug persisted for three hours. Two oscillation phases were recorded in the medial group of mesencephalic reticular nuclei and the lateral nucleus of the hypothalamus: a short positive phase and a prolonged negative one. In other brain structures only negative waves were recorded. A significant functional rearrangement of correlative connections of brain structures took place in 90 minutes after the drug administration. The factor analysis showed that the most subtle connections were preserved in the neocortex and the dorsal hippocampus.

Animals↗