Summary
Activation and aggregation of platelets, as to their biochemical nature, are two distinct partial mechanisms of platelet reaction. The known inhibitors of platelet aggregation such as acetylsalicylic acid or prostacyclin interfere in metabolic pathways involved in the activation of platelets. In contrast, selective inhibitors of aggregation inhibit the interactions between the surfaces of activated platelets. N-acetylneuraminic acid is an example of a selectively antiaggregating substance in vitro. Besides its inhibitory effect on the primary aggregation, a platelet-specific inhibition of prostaglandin synthesis belongs to its pattern of effects. By inhibiting the mechanism of aggregation, N-acetylneuraminic acid also inhibits one of the most important trigger of prostaglandin synthesis in platelets. This results in an interruption of the feedback amplification in activation which is mediated by prostaglandin and thromboxane synthesis in human platelets. These properties of anti-aggregating agents combine a favorable pattern of effects with a platelet-specific point of attack.
Zusammenfassung
Aktivierung und Aggregation der Thrombozyten sind zwei in ihrer biochemischen Natur unterscheidbare Teilmechanismen der Thrombozytenreaktion. Die bisher bekannten „Aggregationshemmer“ wie Acetylsalicylsäure oder Prostazyklin greifen in Stoffwechselprozesse bei der Aktivierung der Thrombozyten ein. Eine selektive Aggregations-hemmung beruht dagegen auf einer Hemmung der Interaktion zwischen den Oberflächen aktivierter Thrombozyten. N-Acetyl-neuraminsäure ist ein Beispiel für eine selektiv anti-aggregierende Substanz in vitro. Zu ihrem Wirkungsmuster gehört neben der Hemmung der primären Aggregation eine für Thrombozyten spezifische Hemmung der Prostaglandin-Synthese. Mit einer Hemmung des Aggregationsmechanismus wird zugleich einer der wichtigsten Auslösemechanismen der Prostaglandin-Synthese gehemmt. Daraus resultiert eine Unterbrechung der Rückkopplungsverstärkung der Aktivierung, die in menschlichen Thrombozyten durch Prostaglandin- und Thromboxan-Synthese vermittelt wird. Diese Eigenschaften anti-aggregierender Substanzen verbinden ein günstiges Wirkungsmuster mit einem thrombozytenspezifischen Angriffspunkt.
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Patscheke, H. Selektive Aggregationshemmung — Ein neues Konzept für Hemmstoffe der Thrombozytenfunktion. Klin Wochenschr 59, 451–457 (1981). https://doi.org/10.1007/BF01695899
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DOI: https://doi.org/10.1007/BF01695899