Antiplatelet therapy: thrombin receptor antagonists
نویسندگان
چکیده
منابع مشابه
Thrombin Receptor Antagonism in Antiplatelet Therapy
Activated platelets play a crucial role in the pathogenesis of atherothrombotic disease and its complications. Even under treatment of antiplatelet drugs, such as acetylsalicylic acid and P2Y12 antagonists, morbidity and mortality rates of thromboembolic complications remain high. Hence, the therapeutic inhibition of protease-activated receptor (PAR)-1, which is activated by thrombin, is a nove...
متن کاملP2Y12 receptor antagonists: a rapidly expanding group of antiplatelet agents.
Adenosine-50-diphosphate (ADP) plays a key role in platelet function, because, although ADP itself is a weak platelet agonist, when secreted from the platelet dense granules where it is stored, it amplifies the platelet responses induced by other platelet agonists. The transduction of the ADP signal involves both a transient rise in free cytoplasmic calcium mediated by the Gq-coupled P2Y1 recep...
متن کامل"Mirror image" antagonists of thrombin-induced platelet activation based on thrombin receptor structure.
Platelet activation by thrombin plays a critical role in hemostasis and thrombosis. Based on structure-activity studies of a cloned platelet thrombin receptor, we designed two "mirror image" antagonists of thrombin and thrombin receptor function. First, "uncleavable" peptides mimicking the receptor domain postulated to interact with thrombin were found to be potent thrombin inhibitors. Second, ...
متن کاملAnti-platelet therapy: ADP receptor antagonists
The P2Y(12) receptor on platelets with which ADP interacts has an important role in promoting platelet function and thereby platelet involvement in both haemostasis and thrombosis. Agents that act as antagonists at this receptor are thus likely to provide effective antithrombotic therapy, provided that there are no adverse effects on haemostasis. Here we describe the ADP receptor antagonists th...
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ژورنال
عنوان ژورنال: British Journal of Clinical Pharmacology
سال: 2011
ISSN: 0306-5251
DOI: 10.1111/j.1365-2125.2010.03884.x