Ex?vivo and In?vivo Antithrombotic Effect of Triflavin, an RGD?containing Peptide
Journal
Journal of Pharmacy and Pharmacology
Journal Volume
46
Journal Issue
1
Pages
58-62
Date Issued
1994
Author(s)
Sheu J.R.
Abstract
Abstract— Triflavin, an Arg?Gly?Asp?containing snake venom peptide, inhibits platelet aggregation through the blockade of fibrinogen binding to the activated platelets. It binds to fibrinogen receptors associated with the glycoprotein IIb/IIIa complex with a Kd value of 7 × 10?8 m. In this study, we found that 125I?triflavin reached the maximal binding to human platelets within 5 min at 25°C. In addition, when triflavin was intravenously administered at 1·0 mg kg?1 to rabbits, it reversibly impaired the platelet aggregation of platelet?rich plasma caused by ADP (20 μm) ex?vivo over 30 min. The platelet counts of the experimental rabbits remained unchanged. Triflavin was effective in reducing the mortality of ADP?induced acute pulmonary thromboembolism in mice when administered intravenously at a dose of 2 μg g?1. Therefore, triflavin was proven to be an effective antithrombotic agent in preventing ADP?induced acute pulmonary thromboembolism in mice and impairing reversibly the platelet function of rabbits when given intravenously. 1994 Royal Pharmaceutical Society of Great Britain
SDGs
Other Subjects
adenosine diphosphate; anticoagulant agent; antithrombocytic agent; arginylglycylaspartic acid; fibrinogen; fibrinogen receptor; snake venom; triflavin; trigramin; unclassified drug; animal experiment; animal model; article; binding competition; controlled study; dose time effect relation; drug efficacy; drug receptor binding; human; human cell; intravenous drug administration; lung embolism; mortality; mouse; nonhuman; rabbit; temperature; thrombocyte activation; thrombocyte aggregation; thrombocyte count; thrombocyte function; thrombocyte rich plasma; Adenosine Diphosphate; Amino Acid Sequence; Animal; Blood Platelets; Crotalid Venoms; Fibrinogen; Fibrinolytic Agents; Human; In Vitro; Iodine Radioisotopes; Mice; Mice, Inbred ICR; Molecular Sequence Data; Peptides; Platelet Aggregation; Platelet Aggregation Inhibitors; Pulmonary Embolism; Rabbits; Support, Non-U.S. Gov't
Type
journal article