Zusammenhänge zwischen Konstitution und Wirkung bei Hemmstoffen der Fibrinolyse

Lohmann, K; Markwardt, F; Landmann, H

doi:10.1055/s-0038-1654795

Cited by 14 publications

(4 citation statements)

References 2 publications

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“…This problem of therapeutic interference with fibrinolysis was solved satisfactorily with the development of synthetic antifibrinolytics -such as e-aminocaproic acid (EACA), aminomethylcyclohexane carboxylic acid (AMCA) andp-aminomethylbenzoic acid (PAMBA) (4,11,16).…”

Section: Inhibitors O F Fibrinolysismentioning

confidence: 99%

Pharmacological Control of Hyperproteolytic States in Blood by Synthetic Inhibitors of Serine Proteinases

Markwardt¹

1978

Pathophysiol Haemos Thromb

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Proteolytic enzymes participate extensively in coagulation, fibrinolysis, kininogenesis, and complement activity. Synthetic low molecular weight inhibitors of these enzymes which belong to the group of serine proteinases allow pharmacological control of these processes. The development of such inhibitors and their therapeutic importance are reported, especially on the pattern of benzamidine derivatives.

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Section: Inhibitors O F Fibrinolysismentioning

confidence: 99%

Pharmacological Control of Hyperproteolytic States in Blood by Synthetic Inhibitors of Serine Proteinases

Markwardt¹

1978

Pathophysiol Haemos Thromb

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“…Die Antifibrinolytika EACA, P AMBA und AMCA sind chemisch ahnlich strukturierte Verbindungen. Sie besitzen je eine endstandige Karboxyl-und Aminogruppe, die in einem Abstand von ungefahr 7 A voneinander angeordnet sind (2,5). Der Mechanismus, durch welchen die Hemmung des Fibrinolysevorganges zustandekommt, ist deshalb bei diesen Verbindungen der gleiche.…”

Section: Besprechungunclassified

Vergleichende Untersuchungen über Antifibrinolytika

Markwardt¹,

Klöckingu²,

Landmann³

1966

Thromb Haemost

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ZusammenfassungDie Wirkung der in der Therapie verwendeten Antifibrinolytika ε-Aminocapronsäure (EACA), p-Aminomethylbenzoesäure (PAMBA) und 4-Amino-methyleyclohexanearbonsäure-( 1 ) (AMCA) wurde in tierexperimentellen und klinischen Untersuchungen vergleichend geprüft. Dabei zeigte sich, daß die zyklischen Aminocarbonsäuren mehrfach stärker wirksam sind als EACA. Ferner wurden Resorption und Ausscheidung der Antifibrinolytika in Tierexperimenten und am gesunden Menschen untersucht.In biochemischen Versuchen wurde neben der Hemmwirkung dieser Verbindungen auf die Plasminogenaktivierung auch ihr Einfluß auf den Fibrinogenabbau durch Plasmin und Trypsin studiert. Hierbei ergab sich, daß PAMBA eine Antitrypsin-und Antiplasminwirkung besitzt, welche diejenige von AMCA und EACA übertrifft.

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“…The action of the synthetic antifibrinolytics s-aminocaproic acid (EACA) (Okamoto 1959;Okamoto et al 1959), p-aminomethylbenzoic acid (PAlVIBA) (Lohmann et al 1963(Lohmann et al , 1964, and trans-4-aminomethylcyclohexane carboxylic acid (trans-AMCHA) (Melander et al 1964;Okamoto et al 1964) is generally thought to be caused by an inhibition of the activation of the fibrinolytic enzyme, plasmin, from its inactive precursor plasminogen. This "antiactivator activity" of the antifibrinolytics was first described by Alkjaersig et al (1959) and repeatedly confirmed later (for review see Markwardt and Landmann 1967).…”

Section: Introductionmentioning

confidence: 99%

Studies on the Mechanism of Action of Synthetic Antifibrinolytics

Landmann¹

1973

Thromb Haemost

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SummaryWhen compared with derivatives of benzamidine, the synthetic antifibrinolytics EACA, PAMBA, and trans-AMCHA are weak competitive inhibitors of ester hydrolysis by urokinase, of plasminogen activation by urokinase and streptokinase, and of plasmin action on synthetic substrates, casein, and fibrinogen. In contrast, the inhibitory effect of the antifibrinolytics equal or surpass, that of benzamidine derivatives on the process of fibrin dissolution by plasmin and on plasma clot lysis. Degradation of fibrin monomers by plasmin seems to be equally strongly inhibited by the antifibrinolytics. Thus, fibrin and fibrin monomers are plasmin substrates, the hydrolysis of which is inhibited by the antifibrinolytics in a different way from their other inhibitory effects on plasmin. It is concluded that this activity accounts for the strong action of these inhibitors on the whole process of fibrinolysis.Plasmin, in contrast to other proteolytic enzymes, was shown to possess a specific ability to attack fibrin resulting in rapid formation of soluble products from the insoluble substrate. The strong inhibitory effect of the antifibrinolytics is not caused by their reaction with the substrate, fibrin, but by their blocking the specific interaction of plasmin with fibrin.The molecular mechanism of the plasmin-fibrin reaction and its inhibition is discussed.

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Zusammenhänge zwischen Konstitution und Wirkung bei Hemmstoffen der Fibrinolyse

Cited by 14 publications

References 2 publications

Pharmacological Control of Hyperproteolytic States in Blood by Synthetic Inhibitors of Serine Proteinases

Pharmacological Control of Hyperproteolytic States in Blood by Synthetic Inhibitors of Serine Proteinases

Vergleichende Untersuchungen über Antifibrinolytika

Studies on the Mechanism of Action of Synthetic Antifibrinolytics

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