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The influence of variation in the P2Y12 receptor gene on in vitro platelet inhibition with the direct P2Y12 antagonist cangrelor

Thrombosis and Haemostasis, 2010
SummaryNovel P2Y12 inhibitors are in development to overcome the occurrence of atherothrombotic events associated with poor responsiveness to the widely used P2Y12 inhibitor clopidogrel. Cangrelor is an intravenously administered P2Y12 inhibitor that does not need metabolic conversion to an active metabolite for its antiplatelet action, and as a ...
Bouman, HJ, van Werkum, JW, Rudez, Goran, Leebeek, Frank, Kruit, A, Hackeng, CM, van den Berg, JM, de Maat, Moniek, Ruven, HJT   +8 more
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Expression and Localization of Purinergic P2Y12 Receptor in Human Nasal Mucosa [PDF]

Allergology International, 2013
BackgroundExtracellular nucleotides such as ATP and UTP are released from essentially all cells, and they interact with cell surface P2 receptors to produce a broad range of physiological responses.
Hideaki Shirasaki, Nobuhiko Seki, Etsuko Kanaizumi   +2 more
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The Function and Regulation of Platelet P2Y12 Receptor

Cardiovascular Drugs and Therapy, 2021
In addition to the key role in hemostasis and thrombosis, platelets have also been wildly acknowledged as immune regulatory cells and involving in the pathogenesis of inflammation-related diseases. Since purine receptor P2Y12 plays a crucial role in platelet activation, P2Y12 antagonists such as clopidogrel, prasugrel, and ticagrelor have been widely ...
Xiaohua Li, Guoxing Zhang, Xia Cao
openaire   +2 more sources

Switching P2Y12 Receptor Inhibiting Therapies

Interventional Cardiology Clinics, 2017
Antiplatelet therapy with aspirin and a P2Y12 receptor inhibitor is the cornerstone of treatment of patients with atherothrombotic disease manifestations. Switching between P2Y12 inhibitors occurs commonly in clinical practice for a variety of reasons, including safety, efficacy, adherence, and economic considerations.
Fabiana, Rollini, Francesco, Franchi, Dominick J, Angiolillo   +2 more
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Role of P2Y12 Receptor in Thrombosis

2015
P2Y12 receptor is a 342 amino acid Gi-coupled receptor predominantly expressed on platelets. P2Y12 receptor is physiologically activated by ADP and inhibits adenyl cyclase (AC) to decrease cyclic AMP (cAMP) level, resulting in platelet aggregation. It also activates PI3 kinase (PI3K) pathway leading to fibrinogen receptor activation, and may protect ...
Yaqi, Zhang, Si, Zhang, Zhongren, Ding
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Responsiveness to P2Y12 receptor inhibitors

Current Opinion in Cardiology, 2011
This review is aimed at describing the variability in response to P2Y12 inhibitor agents, and to focus on the main tests currently available to assess the responsiveness.There is high interindividual response variability to clopidogrel. Some patients do not respond to the drug; this condition can be due to patient-related factors (poor compliance ...
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Progress in Platelet Blockers: The Target is the P2Y12 Receptor

Journal of Cardiothoracic and Vascular Anesthesia, 2013
The considerable progress in P2Y12-platelet blockers has important perioperative implications due to a family of novel agents beyond clopidogrel. Although prasugrel is more potent than clopidogrel due to more efficient hepatic metabolism, it is limited clinically by its irreversibility and bleeding risks.
Prakash A, Patel, Bernard, Lane, John G T, Augoustides   +2 more
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P2Y12 receptors: structure and function

Journal of Thrombosis and Haemostasis, 2015
The platelet P2Y12 receptor (P2Y12R) for adenosine 5'diphosphate (ADP) plays a central role in platelet function, hemostasis, and thrombosis. Patients with inherited P2Y12R defects display mild-to-moderate bleeding diatheses. Defects of P2Y12R should be suspected when ADP, even at high concentrations (≥ 10 μm), is unable to induce full, irreversible ...
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Biology and Pharmacology of the Platelet P2Y12 Receptor

Current Pharmaceutical Design, 2006
Platelets possess two receptors for ADP, P2Y(1) and P2Y(12). ADP is released from platelet dense granules upon platelet activation by numerous agonists and thereby amplifies platelet responses regardless of the initial stimulus. The P2Y(1) receptor is one of many platelet receptors coupled to Gq and initiates ADP-induced activation.
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P2Y12 receptor inhibition and LPS-induced coagulation

Clinical Science, 2016
Platelets play a major role in the complex interactions involved in blood coagulation via multiple mechanisms. As reported in this issue, Schoergenhofer et al. tested the hypothesis that platelet inhibition by prasugrel, a potent platelet P2Y12 ADP receptor antagonist, attenuates the effect of lipopolysaccharide (LPS) on the blood coagulation system in
David W, Essex, A Koneti, Rao
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