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Eksp Klin Farmakol [journal]
- [Melatonin as a drug: present status and perspectives]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):39-44.
Melatonin, a hormone secreted by the pineal gland and peripheral cells, has very wide spectrum of the pharmacological activity and, as shown by experimental data, may provide universal protection of central nervous system and internal organs from damage. These protective properties of melatonin can be successfully used in therapy of many diseases. However, for some reasons, the use of melatonin in clinical practice is not well founded. In this paper, conditions for establishing therapeutic possibilities of melatonin are discussed, including its complex use with traditional drugs.
- [The role of no-dependent mechanisms in melatonin antioxidant activity during hepatic ischemia-reperfusion in rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):33-8.
The antioxidant effect of melatonin on the blood oxygen transport and prooxidant-antioxidant balance during with hepatic ischemia-reperfusion (HIR) with inhibited NO synthase function has been studied in male Wistar rats. The animals were divided into 4 groups: (1) control; (2) hepatic ischemia (Pringle m., 30 min) and reperfusion for 120 min (HIR, n = 9); (9) HIR with melatonin (10 mg/kg, i.p., 10 min before HIR, n = 9); and (4) same with NO inhibitor (L-NAME, 10 mg/kg) added 5 min before melatonin administration. The indices of blood oxygen transport (p50act, pCO2, pH, pO2, etc.) and prooxidant-antioxidant balance (Schiff bases, conjugated dienes, catalase, retinol, alpha-tocopherol) were measured in blood and liver. HIR in group 1 resulted in higher p50act in mixed venous blood and sever oxidative disturbances: rise of CD and SB, decrease of alpha-T, Ret, and Cat. Melatonin in group 3 significantly improved these changes in p50act and prooxidant-antioxidant balance during HIR, but L-NAME in group 4 partly eliminated this effect. It is concluded that the antioxidant effect of melatonin during HIR is partly associated with NO-depended mechanisms, which can modify blood hemoglobin affinity to oxygen, thus limiting oxygen binding in free-radical processes.
- [Antiaggregation activity of arachidonic acid conjugates with neurotropic peptides proglyprol and semax]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):30-2.
The influence two original derivatives of a therapeutically important peptide, bearing arachidonic acid residue with semax and proglyprol, upon platelet aggregation have been studied in vitro. It is established that both derivatives, in contrast to the parent peptide, possess moderate anti-aggregant properties and produce a dose-dependent decrease in the interplatelet interaction induced by ADP, epinephrine, and arachidonic acid within the concentration range of 0.018 - 1.8 mM. This activity was more pronounced for arachidonoylsemax in comparison with arachidonoylproglyprol.
- [The influence of cytoflavin and cardioxipin on the indices of lipid peroxidation and antioxidant protection in the blood of rat with dyslipidemia]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):27-9.
Comparative tests on nonlinear rats of both sex with model violation of lipid metabolism have been performed in order to study the effects of cytoflavin (1.75 ml/kg or 175 mg/kg with respect to succinic acid) and cardioxipin (52.5 mg/kg) on lipid peroxidation and antioxidant protection indices in the blood. It is established that these preparations cause a decrease in the content of malonic dialdehyde (MDA) in erythrocytes that results in increased antioxidant activity and lipid reserves for peroxidation in the blood.
- [Studying spasmolytic activity of imidazo[1,2-a]azepinium derivatives on isolated strips of rat bladder]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):24-6.
We have performed screening tests for imidazo[1,2-a]azepine derivatives by studying their antispasmodic activity on the isolated strips of urinary bladder of female rats. Test compounds showed the ability to reduce the basal tone of bladder stripes on the background of hyperpotassium constriction (40 mM KCl).
- [The influence of citoflavin on molecular mechanisms of hypertensive encephalopathy development in patients with systolic arterial hypertension]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):18-23.
The molecular pharmacological effects of cytoflavin in patients with hypertensive encephalopathy (HE) and isolated systolic arterial hypertension (ISAH) have been investigated using the following methods: assessment of complaints, 24-hour arterial pressure monitoring, ultrasound diagnostics including echocardiography, measurement of lipid profiles and coagulograms, and molecular phenotyping by MALDI-TOF/TOF-MS. A combination of cytoflavin administration with standard therapy of HE and ISAH led to the most expressed return development of clinical symptoms, restoration of the hemodynamic, structural, and geometrical parameters of cardiovascular system, and normalization of the indices of lipid profiles and coagulograms in comparison to patients with HE and ISAH, which accepted only standard therapy. Molecular mechanisms of cytoflavin action have been revealed, which include control of the activity of cellular signaling pathways by means of intermolecular interactions. The optimized therapy of HE and ISAH is recommended for clinical application, which assumes a combined use of standard therapy and cytoflavin and provides a geroprotective action upon the cardiovascular system.
- [Experimental study of the antiarrhythmic properties of zoniporide]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):13-7.
The antiarrhythmic properties of the Na+/H(+)-exchanger inhibitor zoniporide have been studied in experiments on rats. On the model of 45-min myocardial ischemia followed by 45-min reperfusion, the drug produced a significant (two-fold) decrease in the intensity of post-reperfusion arrhythmias (p < or = 0.05). On the model of 7-min ischemia followed by 5-min reperfusion, zoniporide prevented the development of ventricular fibrillation in 71.43% of cases as compared to control (p < or = 0.05). The drug also increased the threshold of electrical fibrillation by 69.23% and reduced the time to recovery of the heart rhythm by 37.85%.
- [GABAergic mechanism of cerebrovascular effect of the NMDA receptor antagonist MK-801]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):8-12.
NMDA receptor antagonist MK-801 (dizocilpine) increases the local blood flow in the cerebral cortex in rats under transient global ischemia (TGI) conditions to a greater degree than in intact animals. The GABA receptor blocker bicuculline in most experiments eliminates or reduces the MK-801 induced increase in the blood flow after TGI, which is indicative of the participation of GABAergic mechanism of cerebrovascular tone control in the observed MK-801 activity.
- [Role of GABA-A receptors in mechanism of psychotropic action of pyrrol[1,2-a][1,4]diazepines studied using drug discrimination technique in Wistar rats]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(6):3-7.
The role of GABA-A receptors in psychotropic effects of pyrrolo[1,2-a][1,4]diazepine derivatives GMAL-24 and GMAL-27 has been studied on an operant method with liquid reinforcement of drug discrimination in male Wistar rats. It is established that, in substitution tests, GMAL-24 (2, 5, 10 mg/kg) and GMAL-27 (2, 5, 10 mg/kg) do not produce interoceptive effects of phenazepam (1 mg/kg) and fail to inhibit interoceptive effects of corasol (20 mg/kg). The obtained results indicate that pyrrolo[1,2-a][1,4]diazepine derivatives do not exhibit GABA-A receptor-positive modulator properties in vivo.
- [Clinical effectiveness of cytoflavin inclusion in intensive care of patients with combined traumatic brain injury]. [English Abstract, Journal Article]
- Eksp Klin Farmakol 2014; 77(4):42-4.
Autors determine the clinical effectiveness of including cytoflavin in intensive care of patients with severe combined traumatic brain injury. A prospective blind randomized controlled study was conducted on two groups involving 101 participants. In group I (58 patients), the intensive care was standard. In group II (43 patients), the intensive care included cytoflavin which was added beginning with the second day of the post-traumatic period. For this purpose, 10 ml of cytoflavin was dissolved in 200 ml of 10% aqueous solution of glucose and was administered intravenously at a speed of 140 drops (7 ml) per minute within 7 days. The use of cytoflavin in complex intensive care of severe combined traumatic brain injury within two days after injury (with the proper correction of blood circulation and respiration) reduced the number of multiple organ dysfunctions, the number is purulent-septic complications, the time of regress in multiple organ dysfunctions, and the reanimation period in intensive care department on the average by a factor of 1.4 - 1.6 (p < 0.005).