Apart from their role in hemostasis and thrombosis, platelets are involved in many other biological processes such as wound healing and angiogenesis. Percutaneous coronary intervention is a highly thrombogenic procedure inducing platelets and monocytes activation through endothelial trauma and contact activation by intravascular devices. Platelet P2Y12 receptor activation by adenosine diphospha...

Platelet G-protein-coupled receptors influence platelet function by mediating the response to various agonists, including ADP, thromboxane A2, and thrombin. Blockade of the ADP receptor, P2Y12, in combination with cyclooxygenase-1 inhibition by aspirin has been among the most widely used pharmacological strategies to reduce cardiovascular event occurrence in high-risk patients. The latter dual ...

Aims: Dual platelet inhibition using anti-P2Y12 drugs and aspirin is the standard of care in patients after percutaneous coronary interventions (PCI). Prasugrel and ticagrelor have been shown to be more potent than clopidogrel with less high on-treatment platelet reactivity. Whether differences in long-term adherence to these drugs can partly explain different antiplatelet efficacy has not been...

Adenine di-Phosphate (ADP) is an important physiological agonist that plays a vital role in normal hemostasis and thrombosis. The importance of ADP in normal hemostasis is clearly demonstrated in patients suffering from storage pool disease who show excessive bleeding tendencies. It is well established that ADP activates platelets through 3 purinergic receptors, namely P2Y1, P2Y12 and P2X1. The...

The important role of the P2Y12 receptor in amplification of platelet activation and associated responses and the limitations associated with clopidogrel therapy have led to the development of novel inhibitors of this receptor. Three reversibly-binding P2Y12 inhibitors are in phase 3 development, ticagrelor, cangrelor and elinogrel. The pharmacology and clinical trial data for each of these inh...

Microparticles are shed from the platelet membrane upon platelet activation by strong agonists, and they aid in clot formation. As the P2Y1 and the P2Y12 receptors differentially contribute to different platelet functions, we studied the relative contribution of the P2Y1 and P2Y12 receptors to microparticle formation from platelets. The P2Y12 receptor antagonist AR-C 69931MX, but not the P2Y1 r...

Although resistance to the P2Y12 antagonist clopidogrel is linked to altered drug metabolism, some studies suggest that these pharmacokinetic abnormalities only partially account for drug resistance. To circumvent pharmacokinetic complications and target P2Y12 receptor function we applied the direct P2Y12 antagonist 2-methylthio-AMP (2-methylthioadenosine 5'-monophosphate triethylammonium salt)...

The P2Y12 receptor antagonist clopidogrel blocks platelet aggregation, improves systemic endothelial nitric oxide bioavailability, and has anti-inflammatory effects. Since P2Y12 receptors have been identified in the vasculature, we hypothesized that clopidogrel ameliorates angiotensin II (Ang II) -induced vascular functional changes by blockade of P2Y12 receptors in the vasculature. Male Spragu...

INTRODUCTION Ticagrelor, the first direct-acting, reversibly binding oral P2Y12 receptor antagonist, appears to have a favorable efficacy and safety profile. AIMS To update the evidence and provide an overview of the available data on ticagrelor. EVIDENCE REVIEW Peer reviewed articles published and listed under Medline Search, and published updated guidelines for pharmacotherapies in acute ...

Platelet P2Y12 is an important ADP receptor that is involved in agonists-induced platelet aggregation and is an important target for the development of anti-platelet aggregation drugs. Here the effects of thio-analogues of uridine triphosphate (UTP) on ADP-induced platelet aggregation are characterised. Using human platelet rich plasma we demonstrate that UTP inhibits P2Y12 but not P2Y1 recepto...