PubMed Health⌕ Search

Biomedical subjects

M Taskov

Publications and source records attributed to M Taskov.

13 recordsLinked to original sources
PubMed1996

Synthesis, gastroprotective, antisecretory and anti-Helicobacter effect of N-[3-(3-(1-piperidinylmethyl) phenoxy)propyl]-hydroxyacetamide 2-hydroxypropane-1,2,3-tricarboxylate bismuth (3+) complex (MX1)-MX1.

MX1 (N-[3-(3-(1-piperidinylmethyl)phenoxy)propyl]-hydroxyacetamide+ ++ 2-hydroxypropane-1,2,3-tricarboxylate bismuth (3+) complex) is a novel salt of the active metabolite of H2-antagonist roxatidine with a complex of bismuth with citric acid. In a model of ethanol-induced ulcers in male Wistar rats, both roxatidine and the bismuth salt reduced the number and the total length of lesions. Comparison of roxatidine and MX1 at equimolar doses of 160 mumol kg-1 showed a more potent cytoprotective effect of MX1. The potency of anti-secretory and antiacidic effects of MX1 was more than twice that of roxatidine on histamine-stimulated secretion in female Wistar pylorus-ligated rats. Microbiological tests with the reference bismuth preparation De-Nol showed prominent anti-Helicobacter properties of MX1 in-vitro. Both test compounds had similar range of MICs to Helicobacter pylori, from 4 to 64 microgram bismuth mL-1. The cytoprotective, antisecretory, anti-acidic and anti-Helicobacter properties of the new agent MX1 warrant further more extensive pharmacological and clinical trials.

Animals↗
PubMed1996

Computer design and syntheses of antiulcer compounds. 1st communication: N-[3-[3-(1-piperidinomethyl)phenoxy]propyl]amines and benzamides.

Aiming to develop new antiulcer agents, a quantitative structure-activity relationship (QSAR) study on in vitro (pA2) and in vivo histamine H2-receptor antagonistic activity of a series of N-[3-[3-(1-piperidinomethyl)phenoxy]propyl]amines was carried out using the OASIS computer system. The results showed that pA2 increases with the decrease (increase) of electron donor (acceptor) properties of molecules, particularly at the NH-reaction site. The finding is consistent with the assumption for an increase of histamine H2-receptor activity of the antagonists with their ability to form H-bonds with the receptor through NH groups. The correlations with hydrophobicity and related topological indices are consistent with the hypothesis that logP should indirectly reflect receptor interactions. In addition a series of N-[3-[3-(1-piperidinomethyl)phenoxy]propyl]benzamides are synthesized. The theoretically predicted in vitro activities of these compounds were found to be in accordance with in vivo tests (percent of inhibition of gastric juice and acid output [mEq/H+/3 h]).

Animals↗
PubMed1991

Dynamics of lipid peroxidation in isoprenaline-induced myocardiopathy.

The dynamics of lipid peroxidation in isoprenaline-induced myocardiopathy was studied in rats. Spontaneous and Fe(II)- catalyzed generation of malondialdehyde (MDA)-like products and chemiluminescence in the heart, liver and brain homogenates were measured. The increase in the interval between treatment of rats with isoprenaline and their killing up to 48 hours led to an increase in MDA content in the heart. Both spontaneous and Fe(II)-induced chemiluminescence also reached their maxima after 48 hours. These data show that well expressed lipid peroxidation in the rat heart occurs approximately 48 hours after isoprenaline application. Isoprenaline metabolization in the liver leads to generation of activated oxygen species which are able to induce lipid peroxidation in the presence of Fe(II). The treatment of rats with isoprenaline caused well-expressed lipid peroxidation in the brain. The maximum of this process occurred approximately 36 hours after isoprenaline application. The results show that both spontaneous and Fe(II)-induced chemiluminescence might be used for the estimation of lipid peroxidation in rat heart homogenates.

Animals↗
PubMed1989

[The effect of vitaton on a model of isoprenaline myocardiopathy in rats].

The influence of the combined preparation vitaton (Pharmachim) was studied on some functional, biochemical and morphological changes, induced after four-fold subcutaneous administration of 100 mg/kg of isoprenaline. The experiments were carried out on three groups: control nontreated, control treated with isoprenaline and experimental, treated simultaneously with isoprenaline and 500 mg/kg of vitalon, administered orally. The preparation was used 3 days before and 2 days after the administration of isoprenaline. Evaluation of the preparation action was made by the following parameters: ECG in the II standard lead, effect on serum level of cholesterol, triglycerols, cholesterol and lipoproteins with high, low and very low density, enzymic activity of hydroxybutiroldehydrogenase (HBDH), creatinephosphokinase (CPK), aspartataminotransferase (ASAT) and alaninaminotransferase (ALAT). Pathomorphological and morphometric studies of the hearts were performed as well. The results from the conducted experiments showed that vitaton reduced pathological changes in the electrocardiographic recordings as well as the abnormal increase in cholesterol and fractions of lipoproteins with low density. Beside this it lowered considerably the enzymic activity, observed under the influence of isoprenaline. The preparation diminished the area of myocardial damage more than twice, estimated by the index of the myocardial damage. The effect of vitalon on the model of isoprenaline myocardiopathy could be explained by its metabolic action and more exactly by its influence on protein synthesis and on lipid metabolism.

Animals↗
PubMed1989

[Experimental studies on protalmine].

The effect of protein-hydrolysate preparation protalmine was studied on physical endurance and body weight of sexually mature rats. It was established that the preparation in a dose of 500 mg/kg of body weight increased static physical endurance and stability to electric stimuli. The effect was more manifested after oral administration of larger dose (1000 mg/kg of body weight). The body weight was not changed considerably in animals of the control group after one month treatment. It was established in other series of experiments performed on sexually mature rats that protalmine increased physical endurance, while Stark protein, used for comparison, did not affect this parameter considerably. Protalmine did not influence atrophy of seminal vesicles and ventral prostate in castrated young rats, e.g. it had no androgenic effect. After venous administration a slight decrease in arterial blood pressure and retardation of heart rate was manifested within the first 10-15 min. The results from these experiments showed that the protein-hydrolyzate preparation protalmine had marked stimulating action.

Animals↗
PubMed1989

[Moniside (isosorbide-5-mononitrate)--the effect on some changes in a hyperlipoproteinemia mode in rats].

The influence of the preparation moniside (isosorbide-5-mononitrate on some functional, lipid and enzymic changes in a model of hyperproteinemia of rats was investigated. Studies were carried out on 45 male rats, divided into 3 groups: I group-control, nontreated; II group--control treated with cholesterol diet; III group--experimental treated with cholesterol diet and monoside in a dose of 20 mg/kg of body weight orally 6 days a week. The experiment continued 3 months. Changes in general state, body mass, static physical endurance, stability to electric current were described as well as the following lipid parameters: cholesterol (mmol/l), cholesterol in lipoproteins with high density (LHD), cholesterol in lipoproteins with low and very low density (LLD, LVLD), tryglycerols (Tr), free fatty acids (FFA). Changes in enzymic activity of aspartataminotransferase (ASAT), alaninamidotransferase (AlAt), hydroxybutiratdehydrogenase (HBDH) and creatinphosphokinase (CPK). Morphological examinations of heart, aorta, liver, kidneys and adrenal were made as well. The results from the experiments showed that in a model with hyperlipoproteinemia general state of experimental animals was impaired, body mass was reduced, physical endurance and stability to electric current reduced, while cholesterol and LVLD/were increased, AlAt increased mult many times, but HBDH and CPK diminished their activity. Functional possibilities of the organism increased at a slight degree under the influence of monoside. Lipid changes, established after cholesterol diet, did not change substantially, while deviations in enzymic activity were normalized.

Animals↗
PubMed1980

Experimental rheoencephalographic and electroencephalographic investigations on piracetam.

The influence of piracetam (2-oxo-1-pyrrolidine-acetamide, Pyramem) on the cerebral circulation and brain bioelectrical activity of cortex and mesencephalic reticular formation (RF) was studied in acute experiments on cats which were encéphale isolé preparations. The methods of local cerebral rheoencephalography (REG) and electroencephalography (EEG) were used. The following REG parameters were assayed: anacrotic section of the curve and its relative part, amplitude and duration of the wave. The arterial blood pressure was followed continuously. The results show that upon piracetam administration (150 mg/kg i.v.) an improvement of the REG parameters of the cortex and RF is observed-an increase of the amplitude and decrease of the values of the anacrotic section of the curve and its relative part. The changes observed indicate a cerebro-vascular resistance decrease and give indirect evidence of cerebral blood volume increase. EEG data are characterized mainly by an increase of alpha-waves, both of cortex and RF. Suggestions for possible mechanism of action of piracetam are made.

Animals↗
PubMed1980

Effect of aligeron on the resistance of the cerebral and peripheral blood vessels.

The effect of the cinnarizine analogue Aligeron on the resistance of cerebral and peripheral blood vessels was studied in acute experiments on cats and dogs. The resistance of the cerebral vessels was determined directly and indirectly. For direct determination the method of autoperfusion was used. The resistance was calculated indirectly as a quotient of mean arterial blood pressure and internal carotid blood flow. For evaluation of Aligeron effect on the resistance of the peripheral blood vessels and method of autoperfusion of the femoral artery was used. Aligeron was administered i. v. and i. a. In some of the experiments the compound was applied on the background of previously injected dihydroergotamine. Cinnarizine and papaverine were used as reference compounds. The results show that Aligeron decreases considerably the cerebral and peripheral resistance vessels tone, and its effect is higher than those of cinnarizine. For the realization of this effect most probably its direct myotropic action plays the main role. The reduction of its effect after alpha-adrenergic blockade suggests an involvement of some adrenergic blocking properties in its mechanism of vascular action.

Animals↗
PubMed1979

Simultaneous investigation of the cerebral circulation and cortical bioelectrical activity in dogs under the influence of piracetam.

By means of the methods of local cerebral rheoencephalography (REG) and electroencephalography (EEG) the effect of piracetam (1-acetamide-2-pyrrolidone, Pyramem) on cerebral circulation and brain bioelectrical activity was studied in acute experiments on dogs. The following REG parameters were assayed: anacrotic section of the curve and its relative part, amplitude and dicrotic index. The influence of the preparation on the spontaneous EEG was studied by means of surface electrodes, pH, pO2, and pCO2 were determined in blood samples from femoral artery and superior sagittal sinus and arterio-venous differences of O2 (AVD-O2) and CO2 (AVD-CO2) were calculated. The arterial pressure and ECG were followed continuously. The results showed that after piracetam administration (100 mg/kg i.v.) an improvement of the REG parameters is observed: increase of the amplitude and decrease of the values of the relative part and dicrotic index. The changes observed indicated cerebro-vascular resistance decrease and increase of the cerebral blood volume. The AVD-O2 increased and the negative AVD-CO2 decreased. The EEG data indicated an improvement in the functional state of the brain cortex. Suggestions as to mechanism of piracetam effect and the usefulness of the methods were made.

Animals↗
PubMed1978

On the vascular action of crataemon.

The vascular action of crataemon is studied. The effect of the drug on organ blood flow is examined using isotope methods. It is established that under conditions of blood loss, 10 mg/kg crataemon sharply inceases the blood supply to the myocardium and liver. Under the same conditions the blood flow in the kidneys and intestines decreases after administration of the drug. Its effect is weaker in case of normal blood pressure. In the case of perfusion of cat hind legs the flavonoid mixture studied has a biphasic effect manifested in the form of initial brief hypertension, followed by a more prolonged and stronger depressor reaction. In larger oral doses (100 and 200 mg/kg) crataemon increases the resistance of the capillaries and decreases capillary permeability in albino rats. The experiments carried out confirm the predominantly action of crataemon on some vascular regions (heart and liver). It has biphasic effect on peripheral vessels, which may be attributed to the presence of different components. The capillary-tonic action is most probably due to the presence of rutin and rutin-like flavonoids.

Animals↗
PubMed1977

On the coronary and cardiotonic action of crataemon.

Crataemon contains the purified flavonoid mixture of Crataegus monogyna. Flowmetric studies of dog coronary blood flow show that it increases after intravenous application of 2 mg/kg crataemon. This increase is statistically significant and lasts about 30 min, with no significant changes in the heart rate and ECG. In experiments on cats it has been found that only the high crataemon doses have a bradycardic effect. Influence on the blood pressure is insignificant and brief. The minute cardiac volume and the cardiac index increase after all doses tested. The work of the left ventricle is also increased, which is considered to be favourable under conditions of operative shock. The general peripheral resistance is much less inhibited, most active being the highest dose tested.

Animals↗