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At least 253 records · Page 14Linked to original sources
PubMed2005

[Inhibition of nitric oxide synthesis during bacterial shock does not prevent development of resistant hypotension and death in rats].

The study subject was the white rat-males Wistar after intra-peritoneal injection of the mixture of St. aureus and B. pyocyaneus daily cultures in the dose calculated as 1 milliard microbial organisms of each species per 100 g b.w., as well as the vascular preparations isolated from aortas of those rats. The aim is to study nitric oxide role in the development of resistant hypotension under generalization of the purulent infection. Infection of the animals with a mixture of gram-positive and gram-negative cultures led to the development of the pathological process, which can be considered as a septic (bacterial) shock. A primary lowering of the vascular tone caused by depression of the myocardial pump and contractile functions was observed. Injection of methylene blue or NOS blockers (L-NAME, S-methyl-thiourea) to the infected animals in the moment of hypotension development caused only a short-term rise in blood pressure. Survival rate in such animals was significantly lower compared to the control infected animals. Repeated injections of those agents hastened death of the experimental animals. The experiments in vitro revealed no dilatory effect of acetylcholine with preserved sensitivity of the vascular preparations to adrenomimetics and exogenous nitric oxide in both control infected animals and animals injected with methylene blue or NOS blockers. The data obtained suggested that resistant hypertension in terminal stages of septic shock is nitric oxide-independent.

Animals↗
PubMedDate not supplied

[Platelet aggregation in modulation of the pathway L-arginine-NO in rats with cerebral ischemia].

Platelet aggregation in the plasma of rats with brain ischemia and modulation of L-arginine-NO pathway were studied in experiments (Born method using analyzer AP 21103AO SOLAR). We used L-arginine and inhibitors of NO-synthase: nonselective inhibitor Nomega-nitro-L-arginine methyl ester, selective inhibitors of neuronal NO-synthase-7-nitro-indazole and selective inhibitor of inducible NO-synthase-S-methylisothiourea. We found that an increase in platelet aggregation in rat plasma observed in both periods is mediated via NO: in an early period of brain ischemia it depends on neuronal NO-synthase and in a late period--on inducible NO-synthase. Moreover, a nonselective inhibitor of all isoforms of NO-synthase (including endothelial NO-synthase) Nomega-nitro-L-arginine methyl ester possesses proaggregant properties. On the other hand, L-arginine in combination with 7-nitro-indazole and S-methylisothiourea induces maximal antiaggregatory effect. These data allows us to suppose that endothelium-derived NO decreases platelet aggregation in brain ischemia-reperfusion in rats.

Animals↗
PubMed2006

NO-synthase inhibitors provide influence on protective effect of modified endotoxine diphosphoryl lipid A in a rat heart model of ischemic-reperfusion injury.

The present study was designed to assess whether a protective effect of the modified diphosphoryl lipid A (modLA) against myocardial ischemia-reperfusion injury (IRI) in rats can be related to the mechanism involving inducible nitric oxide synthase (iNOS). Pre-treatment with modLA significantly reduced the duration of both ventricular tachycardia (p < 0.01) and ventricular fibrillation (p < 0.001) compared to controls. Under these conditions the incidence of animal death was reduced (p < 0.05). The beneficial effect of modLA was markedly attenuated by the prior administration of selective iNOS inhibitor S-methylisothiourea (SMT). In this animal group, mortality was significantly increased (p < 0.01) partially in consequence of sustained ventricular arrhythmias. These results indicate that induction of iNOS can be responsible for cardioprotection of modLA.

Animals↗
PubMedDate not supplied

[Effect of ethyron on carbohydrate metabolism in the myocardium].

Tests staged on rats showed the hypertensive drug ethyron (ethylisothiuronium) to intensify the activity of the oxidative system and pentose cycle in the myocardium, to increase the pyruvate content, raise the redox potential of the lactate-pyruvate potential, to reduce the amount of lactate, heighten the activity of the lactate, malate dehydrogenases, glucose-6-phosphate and cytochrome-c-oxydase. In an isolated spontaneously contracting atrium ethyron abolished the suppressing effect of carbohydrate metabolism inhibitors (sodium fluoride and copper sulphate) on the intensity and frequency of contractions.

Animals↗
PubMed1977

In vivo investigation of antibacterial ointments.

The clinically used topical antibiotic ointments, gentamicin 0.1%, oxytetracycline 3% w/polymyxin 0.1% and chloramphenicol 2% and an experimental preparation, 10-undecen-1-yl thiopseudourea iodide (AHR-1911) were studied for anti-infective action applied externally on the skin of mice inoculated subcutaneously with S. aureus and E. coli. In both infections statistically significant difference was encountered between curative and "clinical" healing rate in the case of the less effective preparations and/or dosages. The method appears suitable to establish and to compare the in vivo activity of ointments. This is not directly related to that of the aqueous drug solutions. AHR-1911, a powerful inhibitor of nucleic acid and protein synthesis, showed a bimodal action, with maximal effectiveness at 0.12-0.25% concentration, due presumably to the anti-inflammatory effect of higher concentrations. Direct evidence for the absorption of the drug from the application site was obtained using 14C labeled AHR-1911.

Abscess↗
PubMed1989

S-aryl (tetramethyl) isothiouronium salts as possible antimicrobial agents, IV.

The 1-octanol/water partition coefficients of a series of antimicrobial S-aryl(tetramethyl)isothiouronium salts, were determined. The concentration of the solute in the two phases was measured by means of HPLC. The values of the hydrophobic parameters thus obtained were correlated to the corresponding capacity factors (log Kw) and compared with those expected on the basis of additive-constitutive principles. The deviations were interpreted quantitatively on the basis of electronic interactions of the substituents in the benzene ring. Equations correlating structural features and antimicrobial activity of some studied compounds by means of molecular parameters were formulated.

Anti-Bacterial Agents↗
PubMed1977

Studies on the topical action of 10-undecen-1-il thiopseudourea iodide (AHR-1911) in acute and chronic dermatitis.

As a follow-up of a preliminary trial, the therapeutic results obtained in 40 cases of acute and chronic dermatitis by the topical application of 10-undecen-1-yl-pseudothiourea hydroiodide (AHR-1911) in an evanescent vehicle containing triethanolamine stearate are presented. The treatment led to complete remission in 14/40 and to favorable results in 18/40 cases. In 2 out of 3 cases of infantile atopic dermatitis improvement was followed by relapse. The responsiveness to AHR-1911 of patients with delayed hypersensitivity, which requires steroids for treatment, is considered of clinical importance. The prompt action of the drug in acute dermatitis, such as is produced by insect-bites, appeared to be impressive. None of the total of 50 cases treated by the author with this new preparation showed any manifestation of intolerance or reaction to the drug.

Acute Disease↗
PubMed1988

S-Aryl(tetramethyl)isothiouronium salts as possible antimicrobial agents--III.

A series of S-Aryl(tetramethyl)isothiouronium salts were prepared and evaluated in vitro for antimicrobial activity. Some compounds revealed interesting inhibiting action on Gram-positive bacteria which is noteworthy in view of the large number of strains antagonized and of the low MIC values. The possible influence of decomposition kinetics to the corresponding mercaptoderivatives was intestigated and compared with those of salts previously studied.

Anti-Bacterial Agents↗
PubMedDate not supplied

[Influence of hypertensive substances on the kallikrein-kinin system of the blood].

It is shown that following a one-time intravenous administration to rats of ethyron, epinephrine and pituitrin (in doses causing hypertension) the amount of the blood plasma kininogen is more than halved with concurrently increasing caseinolysis. A two-day long introduction of these substances activates prekallicrein and brings down the level of the kallicrein inhibitors, whereas a 10 and 20-day coursewise administration of these compounds intensifies the synthesis of some components in the kallicrein-kinine system.

Animals↗
PubMedDate not supplied

[Application of the methods of the mathematical theory of experiments to the development of multicomponent radioprotective preparations].

A study was made of the possibility of using a mathematical theory of experiment in developing effective many-component radioprotective preparations. The preparations composed of cystamine or S-(omega-aminopropyl)-beta-aminoethyl thiophosphate, as the basis, and mexamine, ethyron and gutimine were used as an example to prove the adequacy of such an approach in solving the problems of optimization of composing the radioprotective complexes according to their efficiency and toxicity.

5-Methoxytryptamine↗
PubMedDate not supplied

[Effect of fentolamin and its combination with etiron on microcirculation].

It has been shown in experiments on rats anesthetized with thiopental that intravenous injection of phentolamine in a dose of 10 mg/kg enlarges the microvessels of the mesoappendix, pia mater, liver and kidneys and raises the number of functioning capillaries. Administration of etiron after phentolamine stabilized AP and corrects microcirculation. The drug raises the tone of the microvessels when applied locally in a dose of 0.15 ml (1 : 5000) or intravenously in a dose of 20 mg/kg. Etiron largely produces the constriction of the distal vessels of the arterial area of the microvascular bloodstream. The diameter of the microvessels diminished to a greater degree after intravenous injection of etiron in the presence of a alpha-adrenoreceptor blockade as compared to local application. The sensitivity of the microvessels to etiron administered after phentolamine is inversely proportional to their diameter. Combined use of etiron with alpha-adrenoblockers considerably widens the possibilities of drug control of the vascular tone.

Animals↗