Antithrombotic activity, bleeding effect and pharmacodynamics of a succinyl derivative of dermatan sulphate in rabbits
| Autor: | B. Crepon, M. Level, Pierre Sie, Jean-Claude Lormeau, Bernard Boneu, M. Petitou, Georges Houin, C. Caranobe, Sylvie Saivin |
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| Rok vydání: | 1992 |
| Předmět: |
medicine.medical_specialty
Bleeding Time Dermatan Sulfate Chondroitin sulfate B Thrombin Internal medicine Antithrombotic Animals Medicine Thromboplastin Blood Coagulation Heparin cofactor II Volume of distribution Dose-Response Relationship Drug medicine.diagnostic_test business.industry Succinates Hematology Thrombophlebitis Rats Endocrinology Pharmacodynamics Rabbits business Partial thromboplastin time medicine.drug |
| Zdroj: | British Journal of Haematology. 80:509-513 |
| ISSN: | 1365-2141 0007-1048 |
| DOI: | 10.1111/j.1365-2141.1992.tb04565.x |
| Popis: | Summary This paper compares the pharmacological properties of a new succinyl dermatan sulphate derivative (Suc-DS) to those of the natural dermatan sulphate (DS). Suc-DS was on average 2–3 times more potent than DS in catalysing the inhibition of thrombin by heparin cofactor II and in prolonging the activated partial thromboplastin time and the thrombin clotting time. After bolus injection. Suc-DS was also 2–3 times more potent than DS to prevent experimental venous thrombosis in a Wessler model. Thromboplastin or human serum were used as the thrombogenic stimulus. In contrast, the bleeding effect assessed by rat tail transection technique was comparable. After bolus intravenous injection, the pharmacodynamics of Suc-DS indicated a lower volume of distribution, which was close to the plasma volume, and a slightly lower clearance of elimination. Therefore this chemical alteration of natural DS yields a new compound with an improved antithrombotic benefit/haemorrhagic risk ratio. |
| Databáze: | OpenAIRE |
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