Arterielle Konzentration, arterio-ven�se Differenz im Coronarblut und Organverteilung von C14-markiertem Lanatosid C nach rascher intraven�ser Injektion

Hj, Bretschneider; Doering, P; Eger, Wilhelm A.; Haberland, G. L.; Kochsiek, K; Mercker, H.; G, Scheler F Schulze

doi:10.1007/bf00738219

Cited by 23 publications

(6 citation statements)

References 19 publications

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“…dipyridamole tended to increase myocardial oxygen consumption (13). The mechanism of the positive inotropic action of dipyridamole is to be described in another paper (19).…”

Section: Effects On the (Lei-eloped Tensionmentioning

confidence: 96%

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Simultaneous Assessment of Effects of Coronary Vasodilators on the Coronary Blood Flow and the Myocardial Contractility by Using the Blood-Perfused Canine Papillary Muscle

Himori

Ono

Taira

1976

Japanese Journal of Pharmacology

113

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Abstract-Effects of 6 coronary vasodilators on the coronary blood flow and the con tractile force of the ventricular muscle were examined simultaneously by injecting these drugs to the arterially blood-perfused canine papillary muscle preparation.All com pounds produced a dose-dependent increase in blood flow rate, and relative potencies determined on the basis of doses producing a 100 increase in blood flow rate, ED100, were in the descending order : nifedipine---verapamil---diltiazem; dilazep--,dipyrida mole>carbochromen, and approximately I : 1 12 : 1;'26 : 1 100: 1/300 : 1;'500. All drugs except for dipyridamole caused a dose-dependent decrease in the developed tension of the papillary muscle, although nifedipine and diltiazem in low doses produced a slight increase. Relative potencies determined on the basis of doses producing a 50°0 decrease in developed tension, ID50, were as follows : nifedinine (1), verapanil (1/13), diltiazem (1/40), dilazep (1 100), and carbochromen (1,'270). Ratios of the 1D50 to ED100 were as follows : diltiazem (5.2), nifedipine (3.5), verapamil (3.5), dilazep (2.5), and carbochromen (1.8). The higher the value the more predominant on the coronary vascular bed or the less depressant on the myocardial contractility were their actions.A coronary vasodilator, dipyridamole has no cardiodepressant action, but does increase the venous return and the cardiac output in the dog (1). This suggests that dipyridamole may have rather a cardiostimulant action. In contrast to dipyridamole, a coronary vaso dilator, verapamil reduces the contractile force of the mammalian myocardium (2), and the mechanism of the action underlying the negative inotropic and vasodilator actions has been generally attributed to a calcium-antagonistic inhibition of the excitation-contraction coupling in the cardiac muscle and vascular smooth muscle fibers (3, 4). A recently-developed coronary vasodilator, nifedipine also exerts a negative inotropic effect on the mammalian myocardium (5, 6, 7) and its mechanism of action has also been ascribed to the calcium antagonism (4, 7).The negative isotropic action of these calcium-antagonistic vasodilators is considered to be favorable for the treatment of ischemic heart disease as the reduction in the myocardial contractile force leads to the decreased myocardial oxygen consumption (4). However, an excess of the negative inotropic action is one of the untoward effects as it produces the congestive heart failure. Thus, it is of value to obtain precise information about the potency producing coronary vasodilation and that affecting the myocardial contractility in each coronary vasodilator.Investigators studying the effects of coronary vasodilators on the coronary circulation

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“…dipyridamole tended to increase myocardial oxygen consumption (13). The mechanism of the positive inotropic action of dipyridamole is to be described in another paper (19).…”

Section: Effects On the (Lei-eloped Tensionmentioning

confidence: 96%

“…Diltiazem has a negative inotropic action on the mammalian ventricular muscle and is thought to be a calcium antagonist (10,11). The mechanism of the vasodilator action of dilazep has been ascribed to potentiation of the action of endogenous adenosine (12) as that of dipyridamole (13). A similar mecha nism of action has been suggested for carbochromen (14,15).…”

mentioning

confidence: 91%

Simultaneous Assessment of Effects of Coronary Vasodilators on the Coronary Blood Flow and the Myocardial Contractility by Using the Blood-Perfused Canine Papillary Muscle

Himori

Ono

Taira

1976

Japanese Journal of Pharmacology

113

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“…Several long-acting coronary vasodilators (5,6,7,8,9,10,11) have been reported to enhance the coronary vascular response to adenosine, and the possible mechanism has been considered to he an inhibition of adenosine deaminase in the tissue (12), a blockade of the permeation of adenosine into erythrocytes (13) and vascular smooth muscle cells (14), and/or an inhibition of adenosine degradation in the lung (15).…”

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confidence: 99%

Enhancement of Coronary Vasodilating Action of Adenosine by Dilazep and Dipyridamole in the Dog

Sano

1974

Japanese Journal of Pharmacology

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Abstract-The mechanism of the augmentation of adenosine action by 1, 4-bis-[3 (3, 4, 5-trimethoxybenzoyl-oxy)-propyl] perhydro-1, 4-diazepine (dilazep I, N, N,) and dipyridamole on the coronary vessel was examined in the dog. Cororary blood flow was measured by applying a Morawitz cannula to the in vivo heart. It was found that the ratio of coronary vasodilating activity of adenosine administered into saphenous vein, right atrium, and left atrium was 1: 1.5: 30, and that coronary vaso dilating actions of adenosine administered into saphenous vein, right atrium, and left atrium after dilazep (10 μg/kg, i.v.) were 15.6, 10.8, and 3.3 times greater than those without dilazep, respectively. After dipyridamole coronary vasodilating actions of adenosine administered into saphenous vein, right atrium, and left atrium were 17.5, 14.3, and 5.4 times greater. These results indicate that augmentation of coronary vasodilating action of intravenously administered adenosine by dilazep or dipyrida mole was mainly exerted at the lung and myocardium, and slightly in the blood, and was due to inhibition of the disappearance of adenosine.It is well known that there is a close relationship between coronary blood flow and myocardial metabolism (1); either an augmentation of the myocardial metabolism or hypoxia of the myocardium results in an increased coronary blood flow.Berne (2) has hypothesized that the metabolic regulation of coronary circulation is mediated by adenosine, which produces a powerful coronary vasodilation. Adenosine is always released in a small amount from the myocardium, and the amount of this adeno sine release is increased in a hypoxic condition (3, 4).Several long-acting coronary vasodilators (5,6,7,8,9,10,11) have been reported to enhance the coronary vascular response to adenosine, and the possible mechanism has been considered to he an inhibition of adenosine deaminase in the tissue (12), a blockade of the permeation of adenosine into erythrocytes (13) and vascular smooth muscle cells (14), and/or an inhibition of adenosine degradation in the lung (15).The objective of this study was to clarify the mechanism of the potentiation of adeno sine by certain long-acting vasodilators. MATERIALS AND METHODSForty-six male dogs, weighing 10 to 13 kg, were used. One hr after s.c. administration of 3 mg/kg of morphine and I g/kg of urethane, these animals were anesthetized with 20 mg/kg ix. of sodium pentobarbital.An endotracheal tube was applied to each animal and

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“…The sensitivity of radioactive analysis allows the investigation of the fate of therapeutic glycoside doses in laboratory animals as well as in humans (Okita, Talso, Curry, Smith & Geiling, 1955;Gonzalez & Layne, 1960;Doherty, Perkins & Mitchell, 1961;Doherty & Perkins, 1962;Marcus, Kapadia & Kapadia, 1964;Marks, Dutta, Gauthier & Elliott, 1964;Lage & Spratt, 1965;Katzung & Meyers, 1965;Abel, Luchi, Peskin, Conn & Miller, 1965;Marcus et al, 1964;Marcus, Peterson, Salel, Scully & Kapadia, 1966). Although the tissue accumulation of radioactive glycosides by a few organs has been studied in whole animals and in humans (Bretschneider et al, 1962;Dutta, Marks & Smith, 1963;Marks et al, 1964;Marcus et al, 1964Marcus et al, , 1966, the uptake of the labelled drugs by isolated organs has not been investigated so far.…”

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confidence: 99%

ACCUMULATION AND RELEASE OF ³H‐DIGOXIN BY GUINEA‐PIG HEART MUSCLE

Kuschinsky¹,

Lahrtz²,

Lüllmann³

et al. 1967

British Journal of Pharmacology and Chemotherapy

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Owing to the availability of radioactively labelled cardiac glycosides the determination of minute amounts of these drugs in biological material can now be carried out. Thus, investigations on the distribution and metabolism of cardioactive glycosides in the living organism have been greatly facilitated. Formerly these compounds could only be administered in toxic amounts in order to obtain tissue concentrations which were sufficiently high for chemical or physicochemical analysis. The sensitivity of radioactive analysis allows the investigation of the fate of therapeutic glycoside doses in laboratory animals as well as in humans (Okita,

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Arterielle Konzentration, arterio-ven�se Differenz im Coronarblut und Organverteilung von C14-markiertem Lanatosid C nach rascher intraven�ser Injektion

Cited by 23 publications

References 19 publications

Simultaneous Assessment of Effects of Coronary Vasodilators on the Coronary Blood Flow and the Myocardial Contractility by Using the Blood-Perfused Canine Papillary Muscle

Simultaneous Assessment of Effects of Coronary Vasodilators on the Coronary Blood Flow and the Myocardial Contractility by Using the Blood-Perfused Canine Papillary Muscle

Enhancement of Coronary Vasodilating Action of Adenosine by Dilazep and Dipyridamole in the Dog

ACCUMULATION AND RELEASE OF ³H‐DIGOXIN BY GUINEA‐PIG HEART MUSCLE

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Arterielle Konzentration, arterio-ven�se Differenz im Coronarblut und Organverteilung von C14-markiertem Lanatosid C nach rascher intraven�ser Injektion

Cited by 23 publications

References 19 publications

Simultaneous Assessment of Effects of Coronary Vasodilators on the Coronary Blood Flow and the Myocardial Contractility by Using the Blood-Perfused Canine Papillary Muscle

Simultaneous Assessment of Effects of Coronary Vasodilators on the Coronary Blood Flow and the Myocardial Contractility by Using the Blood-Perfused Canine Papillary Muscle

Enhancement of Coronary Vasodilating Action of Adenosine by Dilazep and Dipyridamole in the Dog

ACCUMULATION AND RELEASE OF 3H‐DIGOXIN BY GUINEA‐PIG HEART MUSCLE

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ACCUMULATION AND RELEASE OF ³H‐DIGOXIN BY GUINEA‐PIG HEART MUSCLE