The P2 Receptors

Hechler, Béatrice; Gachet, Christian

doi:10.1007/978-3-319-47462-5_14

Cited by 3 publications

(3 citation statements)

References 184 publications

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“…Among extracellular nucleotides, ADP plays a central role in platelet function, although it is a weak platelet agonist only inducing reversible responses including aggregation. Platelets express P2Y1 and P2Y12 receptors, and P2Y12R plays an important role in the activation and the stabilisation of platelet aggregates via PI3K and Akt activation and inhibition of adenylate cyclase (Hechler & Gachet, 2017;Cattaneo, 2019). In the present study, we showed NTG-treatment per se did not affect ADP-induced upregulation of platelet CD62P two hours after NTG administration (Fig.…”

Section: Peripheral Inhibition Of P2y12r On Platelets Mitigate Ntg-induced Migraine-like Painsupporting

confidence: 50%

“…Platelets express P2Y 1 and P2Y 12 receptors. P2Y 12 receptor plays an important role in the activation and the stabilisation of platelet aggregates via PI3K and Akt activation and inhibition of adenylate cyclase (Cattaneo, 2019; Hechler & Gachet, 2017). In the present study, we showed that nitroglycerin treatment per se did not affect ADP‐induced up‐regulation of platelet CD62P 2 h after its administration (Figure 7).…”

Section: Discussionmentioning

confidence: 99%

“…This may also result in disturbed signalling in the CNS (Dukhinova et al, 2018). In the periphery, P2Y 12 receptor is highly expressed on platelets, where the receptor appears to be involved in the expression of various inflammatory factors such as IL‐1β, IL‐6 and TNF‐α: inhibition of the receptor with clopidogrel reduced pro‐inflammatory mediator levels in the plasma, notably IL‐1β, IL‐6 and TNF‐α (Hechler & Gachet, 2017). Clopidogrel was also associated with enhanced phosphorylation of Akt and endothelial NOS (Nylander & Schulz, 2016).…”

Section: Discussionmentioning

confidence: 99%

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Involvement of P2Y₁₂ receptors in a nitroglycerin‐induced model of migraine in male mice

Gölöncsér

Baranyi

Iring

et al. 2021

British J Pharmacology

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Supporting information: 5 Figures, 2 Tables and methods Authors contributions: FG carried out behaviour, IHC, FACS experiments, analysed data, performed statistical analyses, and drafted the manuscript. MB conducted HPLC analysis, AI and LH performed blood pressure and heart rate measurement, and analysed the data. LO carried out confocal microscopy and revised the manuscript. ZB designed experiments and revised the manuscript. BS designed and supervised the study and finalized the paper. All authors read and approved the final manuscript.

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Section: Peripheral Inhibition Of P2y12r On Platelets Mitigate Ntg-induced Migraine-like Painsupporting

confidence: 50%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Involvement of P2Y₁₂ receptors in a nitroglycerin‐induced model of migraine in male mice

Gölöncsér

Baranyi

Iring

et al. 2021

British J Pharmacology

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New Approaches in P2Y12 Receptor Blocker Drugs Use

Fakıoğlu

Yardım-Akaydin

2022

Frontiers in Cardiovascular Drug Discovery

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 Thienopyridine-derived clopidogrel, prasugrel, cyclopentyltriazole pyrimidine-derived ticagrelor, and non-thienopyridine-derived ATP analogue cangrelor block the P2Y12 component of ADP receptors on the platelet surface. This prevents activation of the GPIIb/IIIa receptor complex, thereby reduces platelet aggregation. The platelet activation pathway caused by ADP is blocked by P2Y12, and therefore, these drugs have a crucial role in preventing ischemic complications in patients undergoing acute coronary syndrome, including unstable angina, myocardial infarction, and percutaneous coronary intervention. In addition, the use of P2Y12 inhibitors for secondary prevention has also been focused on in clinical studies. The results of recent studies show a lot of variances in terms of duration of use, dosage, and individualized treatment management. The main concern in the clinical use of P2Y12 is dual antiplatelet therapy (with aspirin and a P2Y12 receptor blocker) following intracoronary stenting to prevent stent thrombosis. However, there are also other multifactorial variables in terms of P2Y12 inhibitor use. In this chapter, current and precise medicines regarding P2Y12 inhibitor use are evaluated, from gene testing to escalation and de-escalation strategies. Taking all these into account, providing appropriate drugs selection considering treatment time, onset time, duration of use, side effect profile, treatment limitations, and evaluating and interpreting differences in clinical use based on randomized trials will shed light on coronary heart disease treatment choice. 

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P2Y12 Inhibition beyond Thrombosis: Effects on Inflammation

Gaussem

Bachelot‐Loza

Nesseler

et al. 2020

IJMS

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The P2Y12 receptor is a key player in platelet activation and a major target for antithrombotic drugs. The beneficial effects of P2Y12 receptor antagonists might, however, not be restricted to the primary and secondary prevention of arterial thrombosis. Indeed, it has been established that platelet activation also has an essential role in inflammation. Additionally, nonplatelet P2Y12 receptors present in immune cells and vascular smooth muscle cells might be effective players in the inflammatory response. This review will investigate the biological and clinical impact of P2Y12 receptor inhibition beyond its platelet-driven antithrombotic effects, focusing on its anti-inflammatory role. We will discuss the potential molecular and cellular mechanisms of P2Y12-mediated inflammation, including cytokine release, platelet–leukocyte interactions and neutrophil extracellular trap formation. Then we will summarize the current evidence on the beneficial effects of P2Y12 antagonists during various clinical inflammatory diseases, especially during sepsis, acute lung injury, asthma, atherosclerosis, and cancer.

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The P2 Receptors

Cited by 3 publications

References 184 publications

Involvement of P2Y₁₂ receptors in a nitroglycerin‐induced model of migraine in male mice

Involvement of P2Y₁₂ receptors in a nitroglycerin‐induced model of migraine in male mice

New Approaches in P2Y12 Receptor Blocker Drugs Use

P2Y12 Inhibition beyond Thrombosis: Effects on Inflammation

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The P2 Receptors

Cited by 3 publications

References 184 publications

Involvement of P2Y12 receptors in a nitroglycerin‐induced model of migraine in male mice

Involvement of P2Y12 receptors in a nitroglycerin‐induced model of migraine in male mice

New Approaches in P2Y12 Receptor Blocker Drugs Use

P2Y12 Inhibition beyond Thrombosis: Effects on Inflammation

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Product

Resources

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Involvement of P2Y₁₂ receptors in a nitroglycerin‐induced model of migraine in male mice

Involvement of P2Y₁₂ receptors in a nitroglycerin‐induced model of migraine in male mice