On structure-related properties of synthetic organic clot-dissolving (thrombolytic) compounds

Autor: Gordon Ens, Kurt N. Von Kaulla
Rok vydání: 1967
Předmět:
Zdroj: Biochemical Pharmacology. 16:1023-1034
ISSN: 0006-2952
DOI: 10.1016/0006-2952(67)90275-4
Popis: Salicylic acid detivatives and various other anionic compounds induce upon dissolution marked fibrinolytic activity in human plasma by activating its fibrinolytic system. Clots formed from such plasma dissolve spontaneously on incubation, even after having been carefully washed. The fibrinolysis-inducing capacity of synthetic organic compounds depends on the type and position of the substitution of the mother compound. The capacity for salicylates and γ-resorcylates increased manyfold with the increase of the bulkiness of the substituent. Above and below an optimal concentration, no fibrinolytic activity is obtained. There is evidence that the synthetic fibrinolytic compounds act basically as inhibitors, possibly by interfering with the activity of an antiactivator, thus freeing the blood activator to activate plasminogen. The synthetic fibrinolytic compounds have a strong affinity for proteins; the major part of them is bound to albumin and lost for the fibrinolysis-inducing process. It is hoped that the synthetic organic fibrinolysis-inducing compounds may be developed into convenient thrombolytic agents.
Databáze: OpenAIRE