Antiplatelet drugs receptor antagonists

Antiplatelet and antithrombotic drugs Aspirin, dipyridamole, ticlopidine Thromboxane A2 receptor antagonists—vapiprost and solutroban... 

Mousa SA. Antiplatelet therapies from aspirin to GPIIb/llla-receptor antagonists and beyond. Drug Disoovery Today 1999 4 552-561. 

Nowadays, drug therapy aims to prevent surface mediated platelet activation through at least 12 months of dual antiplatelet therapy (aspirin and a P2Y12 receptor antagonist). Clopidogrel and tioclopidine are the most commonly used [133]. 

In this assay, immobilized platelets are pretreated with a GPIIb/IIIa antagonist, and any unbound drug is washed away before the perfusion of monocytic THP-1 cells. McCarty et al. (2004) demonstrated that agents with slow platelet off-rates such as XV454 (ti/2 of dissociation = 110 min Kd = 1 nM) and abciximab (ti/2 of dissociation = 40 min Kd = 9.0 nM) that are distributed predominantly as receptor-bound entities with little unbound in the plasma, can effectively block these heterotypic interactions as shown by Abulencia et al. (2001) and by Mousa et al. (2002). In contrast, agents with relatively fast platelet dissociation rates such as orbofiban (ti/2 of dissociation = 0.2 min Kd > 110 nM), whose antiplatelet efficacy depend on the plasma concentration of the active drug, do not exhibit any inhibitory effects as described by Mousa etal. (2002). 

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. 

---