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Eksp Klin Farmakol [journal]
- [Experimental study of pinostrobine oxime biotransformation]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):39-44.
We have experimentally studied pathways of elimination of an oximized derivative of phytoflavonoid pinostrobine by HPLC/mass spectrometry. Four potential metabolites of pinostrobine oxime have been found and there was an attempt to determine their molecular structures on the basis of their fragmentation under positive electrospray ionization conditions. It is established that pinostrobine oxime is removed from the organism mainly unchanged and also in the form of glucuronated derivative.
- [Effect of phytic acid and its derivatives on blood lipid peroxydation state in vitro]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):34-8.
We have studied specific features of lipid peroxydation in whole human blood under the action of aqueous solutions of xymedone (19.6 microM), phytic acid (117.9 microM) and its complex (237.6 microM) synthesized in distilled water and isotonic (0.9%) solution of sodium chloride. The estimated parameters included lipid peroxidation (LPO) rate, total antioxidant potential, superoxide dismutase (SOD) level, and malonic dialdehyde (MDA) level in blood plasma and erythrocytes. It was established that the effect of phytic acid on blood samples includes moderate stimulation of total antioxidant activity and SOD activity with predominant prooxidant effect. The phytic acid--xymedone complex synthesized in distilled water exhibits an antioxidant action, while its synthesis in saline solution yields a prooxidant.
- [Influence of new N,N'-substituted piperazines on thrombin-induced platelet activation]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):28-33.
We have studied the influence of new N,N'-substituted piperazines with variable nature of the linker between piperazine and aromatic cycles (carbonyl group in VR-0411 versus sulfonyl group in VR-0511) on thrombin-induced platelet aggregation, cytoplasmic Ca2+ mobilization in platelets, and P-selectin exposure on the platelet plasma membrane. The inhibitory effect of VR-0511 on platelet aggregation exceeds the effects of the reference compound aspirin and VR-0411 by 35 and 42%, respectively (p < or = 0.01). The effects of test compounds on the mobilization of cytoplasmic Ca2+ in platelets and P-selectin exposure indicate that VR-0411 and VR-0511 inhibit platelet activation in these tests by 28 and 61%, (p < or = 0.01) and 34 and 58% (p < or = 0.01), respectively. The possible targets for VR-0411 and VR-0511 are thromboxane and inositol triphosphate-dependent (IP3 formation) pathways of activation signal transfer.
- [Influence of magnesium deficiency correction on the effectiveness of bronchial asthma pharmacotherapy in children]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):23-7.
We have performed 24-week open-labeled comparative randomized parallel-group study of the basic therapy efficacy of uncontrolled and partly controlled atopic asthma children with magnesium deficiency. The additional correction of magnesium deficiency increases the efficacy of atopic asthma basic therapy. It leads to more pronounced inhibition of local allergic inflammation in respiratory system, decreases the exacerbation frequency (9.5%, p = 0.02), and increases the number of asymptomatic days and the 12-week constant asthma control frequency (71.4%, p = 0.145) as compared to the group without magnesium deficiency correction.
- [Comparative study of the effect of S-amlodipine nicotinate and amlodipine benzylate on the arterial pressure of awake rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):20-2.
We have performed a comparative study of the effects of two calcium channel blockers, S-amlodipine nicotinate and amnlodipine benzylate, on the arterial pressure (AP) of awake rats measured in the tail artery. The results of experiments showed that both preparations produce a statistically significant long-term decrease in the AP of animals. In respect of both strength and duration of the hypotensive effect, S-amlodipine nicotinate somewhat exceeds amnlodipine benzylate.
- [Neuroprotective effect of neiroglutam under conditions of activated free radical oxidation]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):16-9.
The neuroprotective properties of the novel glutamic acid derivative neiroglutam have been studied in vitro and in vivo. Neiroglutam demonstrated the protective action on 6-OH-dopamine neurotoxicity model <MI> in vitro, where free radical oxidation is a basic part of pathogenesis. In control rats, focal brain ischemia caused significant increase in thiobarbituric acid reactive species (TBARS) level and decrease in superoxide dismutase (SOD) enzyme activity. In two-year-old rats, preventive administration of the neiroglutam caused a significant reduction in the TBARS plasma concentration (34.5%, p < 0.05), increased SOD activity, and increased the time of acid-induced hemolysis of erythrocytes (40%, p < 0.05).
- [Periods of post-anesthetic rehabilitation and anesthesia dosage for laparoscopic cholecystectomy: retrospective investigation]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):11-5.
A retrospective descriptive nonrandomized cohort study of 585 anesthesia cards of patients who had undergone planned laparoscopic cholecystectomy showed no effect of the patient age and sex on the length of post-anesthetic rehabilitation period. The doses of sodium thiopental, ketamine, and trimeperidine affect the length of these periods by no more than 12%. Further search for and studying of factors affecting the duration of post-anesthetic rehabilitation is required in order to improve the safety and adequacy of general anesthesia.
- [Treatment of surgical stress response by neuroleptics, leu-enkephalin, glycyl-proline dipeptide, and electroanesthesia in experimental animals]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):7-10.
We have studied the effects of chlorpromazine, acepromazine, droperidol, and transcranial electroanesthesia upon evacuation function of the stomach in piglets and the effects of leu-enkephalin and glycyl-proline upon secretory activity of the stomach in dogs and rats during surgical stress to optimize anesthetic dosage. All pharmaceutical and nonpharmaceutical methods of anesthesia used in the experiments were implemented by actiovating stress-limiting systems in post-operational period. Leu-enkephalin, apart from stimulating the stress-limiting factors of neurohumoral systems of the organism, shifted the vector ratio of aggressive and protective factors of gastric mucosa toward strengthening of the latter. The opposite trends of changes in the secretory activity of the stomach of rats in response to surgical stress can be leveled using glycyl-proline as a component of anesthesia.
- [Electrophysiological study of the effects of topiramate on neocortical neurons in rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(8):3-6.
The effect of topiramate (topamax) on the electrical activity of frontal cortical neurons of neoencephalon was studied by microelectrode techniques in rats. Topiramate upon acute intraperitoneal administration and microionophoretic application dose-dependently reduced the frequency of spike activity within 17 - 30 min after injection at a dose of 40 and 80 mg/kg. At the same time, the agent did not change the membrane rest potential, and the magnitude and form of action potentials. Microionophoretically applied topiramate decreased the excitatory response to electroosmotically applied ethanol at "small doses" (ejected current < 50 nA) and enhanced the neuronal depression induced by ethanol at "large doses" (ejected current > 50 nA). It is suggested that the attenuation of alcohol seeking behavior observed after topiramate administration is due to suppression of ethanol activating effects in neoencephalon neurons, while the alleviation of alcohol withdrawal is associated with the central depressant activity.
- [Neuropharmacology of progesterone]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(7):39-44.
Progesterone and its derivatives, synthesized by glial cells in brain tissue of both female and male organism, produce some important local effects, which do not depend upon specific endocrine function of this sex hormone. Being neurosteroids, these compounds exhibit neuroprotective and psychotropic activities, which can be used in clinical practice.