[Antiradical and NO-inhibiting activities of bet-hydroxy(ethoxy) derivatives of nitrous heterocycles].

The antiradical and NO-inhibiting activities of beta-hydroxy(ethoxy) derivatives of nitrous heterocycles (3-hydroxypyridine, 5-hydroxybenzimodazole, and 6-hydroxy(alkoxy)-benzothiazole) have been studied. The antiradical activity has been studied using a homogeneous hydrophilic chemiluminescent system, and the quenching constants (Ki) have been determined. For the most reactive compound, 4-methylthiobenzimidazolyl-3-hydroxypyridine, Ki = 4.5 x 105 M(-1). The NO-inhibiting activity was estimated on a model of the endotoxin shock of experimental animals using a spin trap of nitric oxide radicals based on complexes of iron with sodium diethyldithiocarbamate. It was found that the compounds at doses of 0.25-1 mmol/kg have both the inhibitory and stimulating action on the production of nitric oxide in the liver of animals. The results obtained suggest that some derivatives of nitrous heterocycles can be used as effective antioxidant preparations.

[Primary and secondary metabolism of winter wheat under cold hardening and treatment with antioxidants].

The content of saccharides and phenolic compounds (including flavonoids and lignin) and the activity of L-phenylalanine ammonia-lyase (PAL, EC 4.3.1.5) were determined in leaves and tillering nodes of winter wheat Triticum aestivum L.) cultivars Inna and Moskovskaya 39, differing in the level of frost resistance. These parameters were determined in three groups of plants--control, hardened, and treated with synthetic antioxidants (ambiol and amerol 2000). Cold hardening increased accumulation of primary and secondary metabolites in tissues but decreased the enzyme activity. Treatment with antioxidants also increased the content of saccharides and phenolic compounds (primarily flavonoids) and PAL activity. These changes were more pronounced in cultivar Inna, which is less frost resistant than Moskovskaya 39.

[Clinical efficacy of permanent cardiac pacing in patients with bradysystolic forms of disturbances of cardiac rhythm and conduction].

From 1996 to 2002 primary implantations of pacing systems because of bradysystolic disturbances of cardiac rhythm and conduction had been carried out in 311 patients. Indications were disturbances of atrioventricular conduction in 168 and sick sinus syndrome in 143 patients. According to type of permanent pacing patients were divided into 3 groups: with single-chamber ventricular on demand pacing (VVI, n=215), with single-chamber atrial pacing (AAI, n=39), and with dual-chamber pacing (DDD, n=57). As characteristics illustrating long term clinical results of permanent pacing we used development of the pacemaker syndrome; development of permanent atrial fibrillation; risk of thromboembolic complications and strokes; progression of heart failure; total, cardiovascular mortality and their structure; 7 year survival.

[The use of implantable cardioverter-defibrillators in patients at high risk of sudden cardiac death].

We have reviewed literature on contemporary views on sudden cardiac death (SCD), detection of category of patients belonging to the group with high risk of SCD, and methods of SCD prevention. Randomized studies on assessment of efficacy of implantable cardioverter-defibrillators (ICD) for primary and secondary prevention of SCD have been reviewed in detail as well. We also present experience with clinical management of patients with ICD in the Main Military Clinical Hospital named after N.N.Burdenko. Primary implantations were carried out in 42 patients (5 women) aged 52.7+/-11.9 (19-80) years for secondary (40 patients) or primary (2 patients) SCD prevention. In most patients etiological factor of life threatening ventricular arrhythmias was ischemic heart disease and indications on myocardial infarction in anamnesis (28 patients). In remaining 14 patients we diagnosed right ventricular arrhythmogenic dysplasia (6 patients), dilated cardiomyopathy (3 patients), hypertrophic cardiomyopathy (2 patients), long QT syndrome (2 patients), and the Brugada syndrome (1 patient). During follow-up (from 2 to 48 months, mean 23.7+/-15.4 months) 2 patients died in 5 and 11 months after ICD implantation. In this period ICD discharges were registered in 27 patients (64%). Only in 2 of them (5%) at subsequent testing of the device the therapy was considered unjustified.

[Effect of cardiac resynchronization therapy on quality of life of patients with chronic heart failure].

AIM: To study quality of life of heart failure patients who underwent cardiac resynchronization therapy. MATERIAL AND METHODS: Cardiac resynchronization devices were implanted to 27 consecutive patients (69.7+/-11.9 years of age) with severe heart failure (NYHA class III-IV). Follow up period was 11.6+/-4.9 months. Changes of parameters of quality of life (measured by questionnaire SF-36), ECHO-characteristics (left ventricular ejection fraction, end-diastolic diameter, end-systolic diameter, pulmonary artery blood pressure, mitral and tricuspid regurgitation), six-minute walk distance were assessed at baseline and in 2, 6, and 12 months after implantation of resynchronization device. RESULTS: Cardiac resynchronization therapy improved quality of life according to physical and emotional scales. Changes of the following hemodynamic characteristics were positive: ejection fraction (from 30.6+/-4,2% at baseline to 43.4+/-5.1, 46.8+/-0.3, 45.7+/-3.4% in 2, 6, 12 months after implantation, respectively), end-diastolic diameter (from 82+/-2 mm at baseline to 76+/-3, 73+/-2, 75+/-4 mm in 2, 6, 12 months after implantation, respectively), end-systolic diameter (from 56+/-2 mm at baseline to 53+/-2, 51+/-1, 52+/-3 mm in 2, 6, 12 months after implantation, respectively), pulmonary artery blood pressure (from 44+/-4 mm Hg at baseline to 35+/-3, 30+/-5, 34+/-4 mm Hg in 2, 6, 12 months after implantation, respectively), mitral regurgitation degree (from 2.8+/-0.2 at baseline to 2.4+/-0.2, 2.3+/-0.1, 2.5+/-0.3 in 2, 6, 12 months after implantation, respectively) and tricuspid regurgitation degree (from 2.5+/-0.1 at baseline to 2.1+/-0.2, 2.1+/-0.1, 2.2+/-0.2 in 2, 6, 12 months after implantation, respectively). Moreover, six minutes walk distance significantly improved (from 212+/-18 m at baseline to 270+/-14, 286+/-17 and 278+/-13 m in 2, 6, and 12 months after cardiac resynchronization device implantation, respectively). CONCLUSION: Cardiac resynchronization therapy improves quality of life of patients with terminal stage heart failure.

[A synthesis of tritium-labeled olanzapine].

A synthesis of olanzapine, 2-methyl-10-(4-methyl-1-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine was carried out, and the conditions for its tritium labeling were optimized, to get a tritium-labeled olanzapine preparation with molar radioactivity of 12 Ci/mmol.

[Interaction of nonelectrolytes, the derivatives of 5-hydroxybenzimidazole, with erythrocyte membrane].

The method of spin probe and scanning electron microscopy were used to study the effects of some new synthetic antioxidants and bioregulators, the derivatives of 5-hydroxybenzimidazole, on the membrane structure and morphology of erythrocytes. Analysis of EPR spectra and electron micrographs revealed that the derivatives with various side substituents affect the membrane structure and shape of erythrocytes in a concentration-dependent manner, the effect correlating with the hydrophobic properties of the side derivatives. It was shown that all the compounds in the concentration range 1.10(-7) - 1.10(-3) M exhibit the echinocytogenic action, the most profound effect being found in the compound with benzyl- and ethoxygroup in sites 2 and 5, respectively. Our data suggest that nonelectrolytes, the derivatives of 5-hydroxybenzimidazole, are located in the outer monolayer of erythrocyte membrane.

[The action of benzimidazole derivative preparations on the formation of DNA-protein cross-links in the UV irradiation of chromatin]. / Deistvie preparatov proizvodnykh benzimidazola na obrazovanie sshivok DNK--belok pri UF-obluchenii khromatina.

Effect of benzimidazole-derivatives on the DNA-protein binding formation was studied after UV-radiation of chromatin. These derivatives were shown to protect chromatin from UV-induced DNA-protein binding formation. Structural analog contained two aminomethyl residuals sensibilized additional binding formation in chromatin. Results suggested, that benzimidazole interacted with DNA, while aminomethyl groups interacted with protein and sensibilized binding of DNA with histone H1.

[Method of calculation of the allowance for deviation from the fixed center-to-center spacing in eyeglasses]. / Sposob rascheta dopuska na otklonenie ot naznachennogo mezhtsentrovogo rasstoianiia v ochkakh.

The author provides evidence for a method of calculating the allowance for deviation from the prescribed spacing on centres in the spectacles. Shows that values of the limit deviations obtained by the method described is compared very favourably with those employed today.

[Functional significance of the left adrenal vein and the gonadal veins]. / Funktsional'noe znachenie levoi nadpochechnikovoi veny i ven polovykh zhelez.

Owing to the investigation of changeability variants of the left adrenal, anastomosis of the inferior diaphragmatic and ovarian (testicular) veins--tributaries of the human left renal vein, three variants in inflow of the left adrenal vein in comparison to the left ovarian (testicular) vein have been revealed. In the first variant, that occurs in 70% of cases, the left adrenal vein flows into the left renal vein by 15 cm more medially from the ostium of the ovarial (testicular) vein. The second variant occurs in 11%. The left adrenal and ovarian (testicular) ostia are situated at the same level. The distance from the hilus renalis to the place, where the ostia mentioned get into the renal vein, is about 39 mm. In the third variant (19%) the left adrenal vein gets into the left renal vein nearer to the hilus renalis than the ovarian (testicular) veins. An average distance from the hilus renalis to the ostium of the left adrenal vein is 33 mm. The second variant, when the left adrenal vein gets into the left renal vein, contributes to appearance of the primary varicocele at the left. When the operation for nephrectomy is made at the left, our data make it possible to recommend a purposeful ligation of the left renal vein more laterally to the ostium of the ovarian (testicular) vein. In 80% this ligation will not disturb the function of the left adrenal vein.

[Preclinical study of the safety of the new Soviet tranquilizer gindarin]. / Doklinicheskoe izuchenie bezvrednosti novogo otechestvennogo trankvilizatora gindarina.

The Soviet plant tranquilizer gindarin (an isoquinoline series alkaloid I-tetrahydropalmatine) isolated from the tubers of Stephania glabra Miers was subjected to a preclinical study. As regards the toxicity measured during a single administration to the laboratory animals, gindarin may be classified with moderately toxic substances. Daily intragastric administration of gindarin to rats in doses of 20 and 60 mg/kg for 3 months is likely to give rise to the changes in functions of the CNS, liver and blood. In doses of 1--50 mg/kg gindarin does not exhibit any allergizing, mutagenic or teratogenic properties. Administration of the drug in doses of 1--50 mg/kg from the 1st to the 20th day of pregnancy has shown it to produce marked embryotoxic action. In view of this fact gindarin is contraindicated in pregnancy.