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1.
Eksp Klin Farmakol ; 60(3): 30-3, 1997.
Article in Russian | MEDLINE | ID: mdl-9324394

ABSTRACT

Rats with various models of hypertension (spontaneous, renal, neurogenic, adreno-regenerative) were used in experiments to study the effect of verapamil on parameters of cardio- and hemodynamics in its two-week oral administration. The antihypertensive effect of verapamil was most expressed in rats with spontaneous model of hypertension and initial hyperkinetic variant of circulation.


Subject(s)
Calcium Channel Blockers/therapeutic use , Hemodynamics/drug effects , Hypertension, Renal/drug therapy , Hypertension/drug therapy , Vasodilator Agents/therapeutic use , Verapamil/therapeutic use , Administration, Oral , Animals , Blood Pressure/drug effects , Calcium Channel Blockers/administration & dosage , Calcium Channel Blockers/pharmacology , Disease Models, Animal , Electroencephalography , Heart Rate/drug effects , Hypertension/physiopathology , Hypertension, Renal/physiopathology , Male , Rats , Rats, Inbred SHR , Renal Circulation/drug effects , Vascular Resistance/drug effects , Vasodilation/drug effects , Vasodilator Agents/administration & dosage , Vasodilator Agents/pharmacology , Verapamil/administration & dosage , Verapamil/pharmacology
2.
Eksp Klin Farmakol ; 56(5): 18-21, 1993.
Article in Russian | MEDLINE | ID: mdl-8312801

ABSTRACT

Experiments on open-chest anaesthetized cats were made to test derivatives of crown ethers, such as benzylase-15-crown-5 and dibenzylase-15-crown-5 for their effects on myocardial ischemia and the functional status of a myocardial ischemic focus in temporary coronary occlusion during coronary spasm induced by dihydroergotamine and during coronary microthrombosis caused by ADP. When intravenously administered in doses of 0.5-15 mg/kg, the tested agents were found to enhance myocardial tolerance to ischemia, depressed ST segment in ischemia induced by coronary occlusion and administration of ATP, and prevented ST-segment depression during coronary spasm.


Subject(s)
Crown Ethers , Ethers, Cyclic/therapeutic use , Myocardial Ischemia/drug therapy , Animals , Cats , Disease Models, Animal , Drug Evaluation, Preclinical , Drug Tolerance , Electrocardiography/drug effects , Ethers, Cyclic/toxicity , Female , Lethal Dose 50 , Male , Mice , Myocardial Ischemia/physiopathology
3.
Eksp Klin Farmakol ; 56(3): 32-4, 1993.
Article in Russian | MEDLINE | ID: mdl-8219987

ABSTRACT

The relationship between the inotropic effect and chemical structure of 15-crown-5 and 18-crown-6 derivatives was studied in experiments in open-chest anaesthesized cats, by using computer-aided analysis. The findings showed that the 15-crown-5 derivatives produced more pronounced cardiotropic effect and they were less toxic than 18-crown-6 derivatives. Computer-aided analysis revealed pharmacophoric groups which are responsible for cardiotropic (negative inotropic) activity in the series of crown ether derivatives.


Subject(s)
Crown Ethers , Ethers, Cyclic/pharmacology , Myocardial Contraction/drug effects , Animals , Cats , Depression, Chemical , Dose-Response Relationship, Drug , Ethers, Cyclic/toxicity , Female , Lethal Dose 50 , Male , Mice , Structure-Activity Relationship
4.
Eksp Klin Farmakol ; 56(3): 30-2, 1993.
Article in Russian | MEDLINE | ID: mdl-8219986

ABSTRACT

Analysis of the component structure of single contractions of papillary muscles in guinea pigs was used to study the effects of the crown ether derivative benzylase-15-crown-5 and the antiarrhythmic agents ethmozine and ethacizine. The negative inotropic effect of these compounds was shown to be associated with limited penetration of calcium ions from the sarcolemmal pool into cardiac cellular myoplasm.


Subject(s)
Anti-Arrhythmia Agents/pharmacology , Calcium Channels/drug effects , Crown Ethers , Ethers, Cyclic/pharmacology , Heart/drug effects , Moricizine/pharmacology , Myocardium/metabolism , Phenothiazines/pharmacology , Animals , Calcium Channels/metabolism , Guinea Pigs , Heart/physiology , In Vitro Techniques , Myocardial Contraction/drug effects , Papillary Muscles/drug effects , Papillary Muscles/physiology , Sarcolemma/drug effects , Sarcolemma/physiology , Sarcoplasmic Reticulum/drug effects , Sarcoplasmic Reticulum/physiology , Time Factors
5.
Acta Physiol Pharmacol Bulg ; 18(1): 27-31, 1992.
Article in English | MEDLINE | ID: mdl-1303017

ABSTRACT

The influence of the azacrown ether derivative benzylaza-15-crown-5 on myocardial tolerance to ischemia and on the functional state of the zone of myocardial ischemia during coronary artery occlusion was investigated in experiments on anaesthetized open-chest cats. The compound tested produced a dose-dependent antiischemic effect and prevented the development of myocardial ischemia. In experiments on isolated guinea-pig papillary muscle benzylaza-15-crown-5 inhibited the first and second components of the isoproterenol-induced muscle contraction. The compound decreased the maximal contraction force and had no effect on the cardiac cycle duration and on the time necessary for reaching maximal tension. It is suggested that the protective effect of benzylaza-15-crown-5 during myocardial ischemia is mediated through the inhibition of calcium release from the sarcoplasmic reticulum.


Subject(s)
Anti-Arrhythmia Agents/therapeutic use , Crown Ethers , Ethers, Cyclic/therapeutic use , Myocardial Ischemia/prevention & control , Animals , Blood Pressure/drug effects , Cats , Electrocardiography/drug effects , Female , Heart Rate/drug effects , In Vitro Techniques , Isoproterenol/pharmacology , Male , Myocardial Contraction/drug effects , Myocardial Ischemia/physiopathology , Papillary Muscles/physiopathology
6.
Farmakol Toksikol ; 54(2): 26-8, 1991.
Article in Russian | MEDLINE | ID: mdl-1884790

ABSTRACT

The effect of verapamil on the functional state of the ischemic myocardium, the myocardial tolerance to ischemia and the processes of urgent adaptation of the heart in the coronary artery occlusion was investigated in the experiments on anesthetized open-chest cats. Verapamil was shown to exert the dose-dependent anti-ischemic action, to increase the myocardial tolerance to ischemia, to suppress the response to the physiological saline infusion and not to change adrenoreactivity of the ischemic myocardium at the coronary artery compression.


Subject(s)
Coronary Disease/drug therapy , Heart/drug effects , Verapamil/pharmacology , Adaptation, Physiological/drug effects , Adaptation, Physiological/physiology , Animals , Cats , Coronary Disease/physiopathology , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Electrocardiography , Heart/physiopathology , Hemodynamics/drug effects , Hemodynamics/physiology , Verapamil/therapeutic use
7.
Farmakol Toksikol ; 53(3): 17-9, 1990.
Article in Russian | MEDLINE | ID: mdl-2387374

ABSTRACT

The effect of ionophore monensin on the main parameters of cardio- and hemodynamics was studied in the experiments on anesthetized cats. Monensin (0.075-0.375 mg/kg) administered intravenously in the increasing doses was shown to produce the dose-dependent elevation of arterial blood pressure, the increase of myocardial contractility and the total peripheral resistance. A single administration of monensin (0.375 mg/kg) was found to exert the two-phase action on the parameters of cardio- and hemodynamics.


Subject(s)
Heart/drug effects , Hemodynamics/drug effects , Monensin/pharmacology , Animals , Cats , Dose-Response Relationship, Drug , Heart/physiology , Hemodynamics/physiology , Injections, Intravenous , Myocardial Contraction/drug effects , Myocardial Contraction/physiology , Time Factors
8.
Farmakol Toksikol ; 51(6): 45-8, 1988.
Article in Russian | MEDLINE | ID: mdl-2976684

ABSTRACT

The effects of verapamil and benzyl-aza-15-crown-5 on pressor reactions of blood pressure and perfusion pressure in the femoral artery after administration of noradrenaline, tyramine, angiotensin amide and stimulation of the femoral nerve were studied in acute experiments on anesthetized cats (pentobarbital sodium, 50 mg/kg). Verapamil (0.5 mg/kg) and benzyl-aza-15-crown-5 (9 mg/kg) suppressed pressor reactions to the nerve stimulation and produced no changes at administration of noradrenaline, tyramine and angiotensin amide. One can suggest that the mechanism of the vasodilating action of verapamil and benzyl-aza-15-crown-5 is due to their inhibitory effect on calcium-dependent release of noradrenaline from terminals of the sympathetic nerves. The search of vasodilating agents in the series of crown-ether derivatives is promising.


Subject(s)
Blood Vessels/drug effects , Calcium Channel Blockers/pharmacology , Crown Ethers , Ethers, Cyclic/pharmacology , Verapamil/pharmacology , Angiotensin Amide/pharmacology , Animals , Blood Pressure/drug effects , Blood Vessels/physiology , Calcium Channel Blockers/toxicity , Cats , Drug Interactions , Ethers, Cyclic/toxicity , Mice , Norepinephrine/pharmacology , Succinylcholine/pharmacology , Time Factors , Tyramine/pharmacology , Vasodilation/drug effects
9.
Farmakol Toksikol ; 51(3): 36-8, 1988.
Article in Russian | MEDLINE | ID: mdl-2970398

ABSTRACT

The cardio- and hemodynamic effects of the derivative of aza-15-crown-5 was studied in acute experiments on anesthetized (ethaminal sodium, 50 mg/kg) cats. At intravenous administration the compound was found to induce hypotension, to dilate arterial vessels, to exert negative ino- and chronotropic effects, to decrease the cardiac output. The pharmacological analysis suggests that the mechanism of the cardiotropic action of the compound is due to its intervention in calcium ion metabolism.


Subject(s)
Cardiovascular Agents/pharmacology , Ethers, Cyclic/pharmacology , Heart/drug effects , Hemodynamics/drug effects , Animals , Cardiovascular Agents/toxicity , Cats , Dose-Response Relationship, Drug , Ethers, Cyclic/toxicity , Mice , Time Factors
10.
Farmakol Toksikol ; 46(3): 41-4, 1983.
Article in Russian | MEDLINE | ID: mdl-6861987

ABSTRACT

Experiments on rats were performed to evaluate the action of diazepam (1 mg/kg), phenazepam (1 mg/kg), meprotan (25 mg/kg), mebicar (500 mg/kg), and phenibut (25 mg/kg) on myocardial function under stress-induced injury. Diazepam, phenazepam and phenibut protected the myocardium from stress by raising the functional reserves of the heart. Meanwhile meprotan and mebicar produced no stress-protective action on the heart under similar conditions.


Subject(s)
Heart/drug effects , Stress, Physiological/drug therapy , Tranquilizing Agents/therapeutic use , Animals , Drug Evaluation, Preclinical , Heart/physiopathology , Heart Rate/drug effects , Myocardial Contraction/drug effects , Rats , Stress, Physiological/etiology , Stress, Physiological/physiopathology
11.
Farmakol Toksikol ; 46(1): 38-41, 1983.
Article in Russian | MEDLINE | ID: mdl-6825816

ABSTRACT

It was shown that meprobamate and phenazepam protect the myocardium from hypoxia and decrease myocardial ischemia during coronary occlusion. Phenibut and mebicar reduce the tolerance to ischemia and increase the degree of ischemic injury to the heart. Diazepam has no effect on these processes.


Subject(s)
Coronary Disease/drug therapy , Heart/drug effects , Hypoxia/prevention & control , Tranquilizing Agents/therapeutic use , Animals , Cats , Drug Evaluation, Preclinical , Female , Hemodynamics/drug effects , Male , Time Factors
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