Mechanisms of action of nafazatrom

Seuter, F; Busse, Wolf D.

doi:10.1016/0049-3848(83)90361-4

Cited by 5 publications

(3 citation statements)

References 11 publications

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“…The drug was also found equipotent in decreasing the size of preformed thrombi in doses comparable to those used to prevent thrombus formation (7). Whereas all investigators agree that the drug has very little, if any, effect on blood coagulation and fibrinolysis (7,(17)(18)(19), there is some controversy regarding its effect on platelet function. Seuter and associates (7) and Seuter and Busse (17) reported that nafazatrom had no effect on platelet function in vitro or ex vivo.…”

Section: Discussionmentioning

confidence: 99%

Platelet Survival and Function in Animals with Prosthetic Mitral Valve: The Effect of Nafazatrom

1984

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SummaryThromboembolism remains a serious problem in patients with prosthetic heart valves. Previous studies documented a number of platelet abnormalities in such patients and correlated the occurrence of thromboembolic complications with short platelet survival. We have studied platelet survival and platelet aggregation in eight goats fitted with prosthetic mitral valves and repeated the studies following treatment with nafazatrom, a potent antithrombotic agent. Eleven survival studies in eight animals showed a platelet survival not significantly different from control (6.52 ± 0.72 vs. 6.94 ± 0.81 days). Following seven to ten days of oral drug administration, platelet survival in the test animals was 7.34 ± 0.96 days, significantly longer than pretreatment results (p <0.01). Animals with the shortest pretreatment platelet survival achieved substantial prolongation of platelet life span following drug treatment. The drug caused no change in ex vivo platelet aggregation.

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Section: Discussionmentioning

confidence: 99%

Platelet Survival and Function in Animals with Prosthetic Mitral Valve: The Effect of Nafazatrom

1984

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“…The drug significantly increased PG12 release from rat aortic rings (9,11,41,63,70). These observations have been confirmed using different treatment regimens (61). The antiaggregatory activity of nafazatrom was correlated with the 6-keto-PGF,, levels measured by NAFAZATROM I75 radioimmunoassay (60).…”

Section: Prostacyclin Generationmentioning

confidence: 56%

“…Nafazatrom effects include its ability to act as a reducing cosubstrate for the hydroperoxide transformation (19,28, 44,61,64). Nafazatrom has no effect on the conversion of prostaglandin H2 (PGH2) to PG12 but protects the prostacyclin synthetase from inactivation by hydroxyperoxyeicosatetraenoic acid (HPETE) and accelerates the conversion of prostaglandin G2 to PGH2.…”

Section: Efsect Of Nafazatrom On Cyclooxygenase and Lipoxygenase Pathmentioning

confidence: 99%

Nafazatrom*

Seuter¹,

Fiedler

Philipp

1986

Cardiovascular Drug Reviews

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Venous thrombosis and pulmonary embolism represent a serious hazard for patients undergoing major surgery. Arterial thrombosis may be the cause of stroke, myocardial infarction, or gangrene. In a search for better drugs for effective and safe short-and long-term prophylaxis, we discovered and evaluated the antithrombotic effects of nafazatrom.Nafazatrom {BAY g 6575, 3-methyl-1 -[2-(2-naphthyloxy)-ethyl]-2-pyrazolin-5-one, Cl6H,d2O2, MW 268) ( Fig. 1) was synthesized by Moller (50). It is relatively insoluble in water at the pH range 4 to 9 but is soluble in organic solvents such as polyethylene glycol, dimethyl sulfoxide, and ethanol. PHARMACOLOGY Freezinglnduced ThrombosisThe activity of nafazatrom on venous thrombosis was assessed by the method of Meng (45,46) and on arterial thrombosis by the methods of Meng and Seuter (48) and Seuter et al. (62).The antithrombotic activity was determined in rats, rabbits, and guinea pigs. In rats and guinea pigs, thrombosis was produced by freezing jugular vein, carotid artery, and in some experiments iliac artery. In rabbits, femoral arteries were injured with a freezing technique (45,46,48). The rat and guinea pig vessels were frozen at -15°C over a length of approximately 1 cm in a metal groove for 2 min and simultaneously compressed by a weight of 200 g. The rabbit vessels were exposed to the temperature of -12°C for a period of 5 min and a compressing weight of 500 g. In addition, arteries were clamped with a small silver clip (width 0.154.20 mm) distal to the lesion. At the end of the experiments the animals were heparinized and anesthetized, and the thrombi were removed from the injured vessel segments. The thrombosis was quantitated either by the wet weight of thrombi immediately after removal or by their hemoglobin content. *Dedicated to Prof. Dr. med. Friedrich Hoffrneister, Wuppertal (FRG), on the occasion of his 60th birthday. 163

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Newer Pharmacological Agents

Yardumian¹,

Machin²

1988

Platelet-Vessel Wall Interactions

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Mechanisms of action of nafazatrom

Cited by 5 publications

References 11 publications

Platelet Survival and Function in Animals with Prosthetic Mitral Valve: The Effect of Nafazatrom

Platelet Survival and Function in Animals with Prosthetic Mitral Valve: The Effect of Nafazatrom

Nafazatrom*

Newer Pharmacological Agents

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