Thrombin antiplatelet effect

Several studies have explored the anti-platelet effect produced by naturally occurring quinones. For example, the quinone fraction isolated from Auxemma oncocalyx (Allem/Eo) is a reversible and concentration-dependent inhibitor of human platelet aggregation induced by ADP, arachidonic acid, collagen and thrombin [298], Zhang et al. [299] studied the antiplatelet effects of 2-chloro-3-(4-acetophenyl)-amino-l,4-naphthoquinone. This... 

Thrombin receptor (protease activated receptor-1) antagonists as potent antithrombotic agents with strong antiplatelet effects 06JMC5389. 

Preclinical Data Supporting the Antiplatelet Effect of Thrombin Receptor Antagonists 1551... 

Chackalamannil, S. (2006) Thrombin receptor (protease activated receptor-1) antagonists as potent antithrombotic agents with strong antiplatelet effects. Journal of Medicinal Chemistry, 49 (18), 5389-5403. 

Chackalamannil, S. (2011) The discovery of vorapaxar (SCH 530348), a thrombin receptor (protease activated receptor-1) antagonist with potent antiplatelet effects, in Accounts in Drug Discovery Case Studies in Medicinal Chemistry, RSC Drug Discovery Series No. 4 (eds J.C. Barrish, P. H. Carter, P.T.W. Cheng, and R. Zahler), Royal Society of Chemistry, Cambridge, UK, pp. 25-49. 

The antiplatelet activity of nitroaspirins NCX-4215 and NCX-4016 was compared in vitro to aspirin with comparable results for maximal inhibition of arachi-donic acid-stimulated platelet aggregation (50). Furthermore, NCX-4016 was more efficient in inhibiting platelet activation induced by thrombin (48, 50). This was reversed by oxyhemoglobin and methylene blue acid, further supporting the NO-related inhibitory effect. NCX-4016 was shown to possess greater antiinflammatory and analgesic activity (51, 52). The antithrombotic activity of NCX-4016 was also present in vivo (53) and reduced pulmonary thromboembolism... 

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