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Eksp Klin Farmakol [journal]
- [Modern notions about the role of taurine in the central nervous system]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):38-44.
Literature data concerning modern notions about the role of taurine in the central nervous system are analyzed. Mechanisms of the neuroprotective activity of taurine are described. Evidence showing the effects of taurine as neurotransmitter, neuromodulator, antioxidant, etc. is provided.
- [Serotonin and its receptors in the cardiovascular system]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):32-7.
Serotonin in cardiovascular system plays an important role in blood coagulation, allergy, and inflammation, as well as in blood vessel tone regulation. In this review, the mechanisms of serotonin effects upon the cells of blood vessels are considered and the list of main agonists and antagonists is presented. The signaling pathways activated by serotonin and their interaction in normal and pathological states are described.
- [Influence of nonsteroidal anti-inflammatory drugs on chemiluminescence of polymorphonuclear leukocytes in patients with intolerance of these drugs]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):28-31.
We have studied the intensity of barium sulfate stimulated luminol- and lucigenin-dependent chemiluminescence (SLCHL and SLCCHL) in polymorphonuclear leukocytes (PML) after pre-incubation of PML suspension with sodium salicylate, sodium metamizole, or sodium diclofenac at various concentrations in healthy donors and patients with intolerance to aspirin, and/or sodium metamizole, and/or sodium diclofenac. No significant differences of SLCHL and SLCCHL indicators in PML isolated from healthy donors and patients with intolerance to these drugs have been found, which indirectly indicates the absence of any specific features in the oxidative metabolism of PML enzymes under the influence of indicated NSAIDs in patients intolerant of these drugs as compared to donors.
- [Preclinical study of the new anti-influenza drug candidate AV0038 (ethyl 2-(dimethylaminomethyl)-5-hydroxy-1-methyl-6-(pyridin-3-yl)-1H-indole-3-carboxylate)]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):23-7.
In the framework of preclinical testing of AV0038, ethyl 2-(dimethylaminomethyl)-5-hydroxy-1-methyl-6-(pyridin-3-yl)-1H-indole-3-carboxylate, which showed high efficiency in the prevention and treatment of influenza A/Aichi/2/69 (H3N2) in mice, we have studied the drug solubility and stability in aqueous solutions, metabolic stability in human liver microsomes, stability in blood plasma of mice and humans, binding to plasma proteins of mice and humans, pharmacokinetics and bioavailability in mice, and the acute toxicity and the maximum tolerated dose. It is established that AV0038 has attractive pharmacological properties as anti-influenza drug candidate. The therapeutic doses of AV0038 do not cause acute toxicity in mice. It is expedient to continue preclinical investigations and study the drug metabolism, metabolites, and sub-chronic toxicity in test animals.
- [Comparative study of the toxicity and antiarrhythmic activity of some organic derivatives of dimethylacetamide]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):20-2.
A comparative study of the acute toxicity and antiarrhythmic activity of new domestic derivatives of dimethylacetamide showed that the introduction of amino and carboxylic acid residues into the structure of compounds is accompanied by reduction of the toxic properties of new substances on the average 2.73 times (p = 0.002) upon intraperitoneal introduction to animals. It has been established that the derivatives are able to prevent the formation of aconitine induced arrhythmias and eliminate the arrhythmia that occurs on the second day of myocardial infarction in dogs. Original derivatives of dimethylacetamide exhibit antiarrhythmic properties and their activity increases in proportion to the acute toxicity (r = 0.83, p = 0.0043).
- [Influence of mydocalm on the degree of intra-abdominal hypertension and local blood circulation in the intestinal wall in experiment]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):15-9.
The effect of mydocalm (tolperison, 5 mg/kg single dose) on the dynamics of intra-abdominal hypertension (IAH), blood circulation regulation, and oxygen balance in the tissues of intestinal wall were studied in acute experiments on rabbits. Using a special stand of original design, the initial IAH level was modeled at 200 mm H2O with the subsequent stopping of further receipt of liquid during 3 hours in an elastic container in the abdominal cavity. During 3-h observation without drug administration, no changes in IAH due to the tone of muscles of the frontal abdominal wall takes place, but there is progressive deceleration of local blood flow (-35.33 + 0.99%, p < 0.01), suppressed dilation (-20.02 + 0.54%, p < 0.01) and constriction (-60.45 + 1.17%, p < 0.01) reactivity of vessels, and decreased oxygen tension (-47.18 + 0.75%, p < 0.01) in the intestinal wall at the end of experiment. The introduction of mydocalm reduces the tone of muscles of the frontal abdominal wall, which leads to a decrease in IAH (maximum effect after 1.5 hours, -20.81 + 0.84%, p < 0.01) and prevents decrease in the local blood flow (-26.77 + 0.41%, p < 0.01), suppression of dilation (-16.51 + 0.34%, p < 0.01) and constriction (-37.85 + 0.61%, p < 0.01) reactivity of vessels, and reduction in oxygen tension (-36.60 + 1.18%, p < 0.01) at the end of experiment. The administration of mydocalm can extend the limits of application of a conservative therapy for patients with IAH and to improve the results.
- [Studying the development of imipramine tolerance and prospects of its overcoming with the aid of tianeptine]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):10-4.
Reaction of two groups of mice to sub-chronic imipramine administration has been studied in a series of experiments, where one (control) group received physiological saline instead of imipramine. Then, both groups were randomly divided to receive either tianeptine (two groups) or physiological saline (two groups) for three days. After this period, the reaction of mice to imipramine was assessed again by measuring the immobilization duration in the tail suspension test. It was found that sub-chronic administration of imipramine (6 days) did not reduce sensitivity of the mice to this medication. Tianeptine showed "pro-depressive" action in the tail suspension test, but the administration of tianeptine increased the sensitivity of rodents to imipramine.
- [Insulin potentiating and antidepressant effects of 3-oxypyridine and succinic acid derivatives]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):6-9.
The dependence of the antidepressant action of 3-oxypyridine and succinic acid derivatives (emoxipine, reamberin, and mexidol) on the insulin potentiating activity of these therapeutic agents has been studied in experiments on rats. Alpha-lipoic acid was used as a reference drug. It was established that single administration of emoxipine, reamberin, mexidol and alpha-lipoic acid in optimal doses, corresponding to the therapeutic range in humans, increased the sensitivity of animals to insulin according to the criterion of insulin coma development. Triple administration of the therapeutic agents studied in the same single dose produced an antidepressant effect according to the criterion of "desperate behavior" in Porsolt forced swimming test. Standardization of obtained data by average difference from the control and further correlation analysis demonstrated that the extent of antidepressant action of emoxipine, reamberin, mexidol and alpha-lipoic acid considerably depends on their insulin potentiating activity (r = 0.762, p = 0.004).
- [Influence of hemantane in injectable dosage form on levodopa-induced dyskinesia in rats with model parkinsonian syndrome]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(5):3-5.
Levodopa-induced heavy dyskinesia was modeled in rats with severe hemiparkinsonian syndrome induced by injection of 6-hydroxydopamine in the left medial forebrain bundle. It is established that the antidyskinetic effect of the injectable dosage form of a new antiparkinsonian drug hemantane (5 mg/kg) after a single intravenous administration is weaker than that of the most effective in clinical practice antidyskinetic drug amantadine (20 mg/kg). However, after five days of treatment, the effect of hemantane injections exceeded that of amantadine.
- [Nephroprotective properties of third-generation beta-adrenoblockers]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(3):40-3.
Experimental and clinical data on the nephroprotector properties of third-generation beta-adrenoblockers nebivolol and carvedilol are reviewed. These properties are related to the antihypertensive effect and ability of drugs to suppress oxidative stress in glomerules, proximal renal tubules, and surrounding interstitial tissue.