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Expression and Localization of Purinergic P2Y12 Receptor in Human Nasal Mucosa
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 +2 more
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The Function and Regulation of Platelet P2Y12 Receptor
Cardiovascular Drugs and Therapy, 2021In 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
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Switching P2Y12 Receptor Inhibiting Therapies
Interventional Cardiology Clinics, 2017Antiplatelet 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 +2 more
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Role of P2Y12 Receptor in Thrombosis
2015P2Y12 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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Progress in Platelet Blockers: The Target is the P2Y12 Receptor
Journal of Cardiothoracic and Vascular Anesthesia, 2013The 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 +2 more
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P2Y12 receptors: structure and function
Journal of Thrombosis and Haemostasis, 2015The 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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Purification and Functional Reconstitution of the Human P2Y12 Receptor
Molecular Pharmacology, 2003The human P2Y12 receptor (P2Y12-R) is a member of the G protein coupled P2Y receptor family, which is intimately involved in platelet physiology. We describe here the purification and functional characterization of recombinant P2Y12-R after high-level expression from a baculovirus in Sf9 insect cells.
Erik T, Bodor +5 more
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Responsiveness to P2Y12 receptor inhibitors
Current Opinion in Cardiology, 2011This 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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P2Y12 receptor inhibition and LPS-induced coagulation
Clinical Science, 2016Platelets 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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Strategies for targeting the P2Y12 receptor in the central nervous system
Bioorganic & Medicinal Chemistry Letters, 2022The purinergic 2Y type 12 receptor (P2Y12R) is a well-known biological target for anti-thrombotic drugs due to its role in platelet aggregation and blood clotting. While the importance of the P2Y12R in the periphery has been known for decades, much less is known about its expression and roles in the central nervous system (CNS), where it is expressed ...
Ben B, Ma +4 more
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