Dosing of Clopidogrel for Platelet Inhibition in Infants and Young Children | Circulation
... effect through an active metabolite that specifically and irreversibly modifies the ADP purinergic P2Y12 platelet receptor and ... and the number of P2Y12 receptors per platelet.. The present study has some limitations. First, although the present study is ... The differences between active-dose level and placebo were estimated within the ANOVA framework with 95% confidence intervals. ... After platelet-inhibition assessments had been completed on a minimum of 3 active patients and 1 placebo patient per age group ...http://circ.ahajournals.org/content/117/4/553
Adenosine diphosphate receptor inhibitor - Wikipedia
The molecular target of the active metabolite of ADP receptor inhibitors is the P2Y12 receptor. P2Y12 receptor is a G-coupled ... The P2Y12 receptor is a surface bound protein found on blood platelets. They belong to G protein-coupled purinergic receptors ( ... The active metabolite, which is R-138727 (thiol intermediate), either binds irreversibly to the P2Y12 receptor or is metabolic ... They are all prodrugs which need to be converted to an active metabolite in-vivo to inhibit the P2Y12 receptor. On the other ...https://en.wikipedia.org/wiki/Adenosine_diphosphate_receptor_inhibitor
METHODS AND COMPOSITIONS FOR THE ASSESSMENT OF DRUG RESPONSE - Patent application
... active metabolites that react with and irreversibly inhibit the platelet P2Y12 adenosine diphosphate (ADP) receptor, which is ... to its platelet receptor (the P2Y12 purinergic receptor) the duration of action is five to ten days which approximates the ... its platelet receptor (the P2Y12 purinergic receptor) and the subsequent activation of ADP-mediated glycoprotein GPIIb/IIIa ... active metabolite. The first step leads to formation of 2-oxo-clopidogrel, which is then metabolized to the active metabolite. ...http://www.patentsencyclopedia.com/app/20110060532
Molecules | Free Full-Text | Action of Natural Products on P2 Receptors: A Reinvented Era for Drug Discovery | HTML
In addition, there were seventeen animal sources that affected P2X7 and P2Y1 and P2Y12 receptors. Natural products have ... and inflammatory and neuropathic diseases having been linked to the participation of purinergic (P2) receptors, there has been ... Of those, nine different plant sources demonstrated effects on P2X2, P2X3, P2X7, and possibly P2Y12 receptor subtypes. ... Microorganisms, which represent the largest group, with 26 different sources, showed effects on both receptor subtypes, ranging ...http://www.mdpi.com/1420-3049/17/11/13009/htm
A Clopidogrel-Insensitive Inducible Pool of P2Y12 Receptors Contributes to Thrombus Formation: Inhibition by Elinogrel, a...
2008) The active metabolite of prasugrel effectively blocks the platelet P2Y12 receptor and inhibits procoagulant and pro- ... 2006) Distinct roles for protein kinase C isoforms in regulating platelet purinergic receptor function. Mol Pharmacol 70:1132- ... To determine whether clopidogrel blocked this inducible pool of P2Y12 receptors, we determined the number of P2Y12 receptors on ... a prodrug undergoing biotransformation to an active metabolite that irreversibly antagonizes P2Y12 receptors (Savi et al., 2001 ...http://jpet.aspetjournals.org/content/339/1/54
New P2Y12 Inhibitors | Circulation
... as a result of competitive interaction between cangrelor and the active metabolite of clopidogrel at the P2Y12 receptor level. ... the Gq-coupled P2Y1 receptor and the Gi-coupled P2Y12 receptor, which belong to the family of purinergic P2 receptors. ... faster P2Y12 receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite ... Figure 1. Central role of P2Y12 in platelet aggregation. ADP, by interacting with P2Y12, a 7-transmembrane receptor that is ...http://circ.ahajournals.org/content/121/1/171
Clopidogrel and Response Variability Investigation Study 2 - Full Text View - ClinicalTrials.gov
... must be converted into an active metabolite that selectively and irreversibly binds to the P2Y12 platelet membrane receptor. As ... Purinergic P2Y Receptor Antagonists. Purinergic P2 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. ... Relationship between active metabolites concentration and IRPA. *Relationship between active metabolites and dose of ... Relationship between active metabolites concentration and IRPA [ Time Frame: during the study ]. *Relationship between active ...https://clinicaltrials.gov/ct2/show/NCT00822666
Elderly Patients With Acute Coronary Syndromes Managed Without RevascularizationClinical Perspective | Circulation
receptors, purinergic P2Y12. Introduction. Optimizing care for elderly patients with cardiovascular disease constitutes both a ... Relationship between exposure to prasugrel active metabolite and clinical outcomes in the TRITON-TIMI 38 substudy. J Clin ... Prasugrel, a thienopyridine P2Y12 inhibitor, has been shown to reduce the risk of ischemic events compared with clopidogrel in ... Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med. 2012;366:20-33. ...http://circ.ahajournals.org/content/128/8/823
P2Y<sub>12</sub> receptor | P2Y receptors | IUPHAR/BPS Guide to...
P2Y receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets. ... the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor. Thrombosis and haemostasis, 94 (3): ... SP1999 , P2YADP , HORK3 , P2Y purinoceptor 12 , P2Y12 platelet ADP receptor , purinergic receptor P2Y ... which found CysLTs to be inactive at the P2Y12 receptor . Thus the interaction of CysLTs with the P2Y12 receptor is ...http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=328
Anti-platelet agents in pediatric cardiac practice Mohanty S, Vaidyanathan B - Ann Pediatr Card
Adenosine diphosphate (ADP), for example, activates purinergic receptor P2Y12 and evokes morphological changes of platelets. ... 1] The active metabolite has an elimination half-life of about 8 hours.. Following an oral dose of Dipyridamole, plasma ... Ticlopidine and clopidogrel are prodrugs and are converted in the liver by cytochrome P 450 enzymes to an active metabolite. ... Ticlopidine and clopidogrel are thienopyridines, which cause irreversible blockade of the ADP receptor (P2Y12) on platelet cell ...http://www.annalspc.com/article.asp?issn=0974-2069
Tailored Antiplatelet Therapy Versus Recommended Dose of Prasugrel - Full Text View - ClinicalTrials.gov
Purinergic P2Y Receptor Antagonists. Purinergic P2 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. ... events and pharmacokinetic data suggests that elderly patients are exposed to a higher concentration of the active metabolite ... Monitoring with VerifyNow P2Y12, 2 weeks after initiation of 5 mg of maintenance dose of prasugrel, reduction of antiplatelet ... Monitoring with VerifyNow P2Y12, 2 weeks after initiation of 5 mg of maintenance dose of prasugrel, reduction of antiplatelet ...https://clinicaltrials.gov/ct2/show/NCT01538446?term=stroke+AND+san+diego&recr=Open&rank=4
The Influence of Smoking Status on Prasugrel and Clopidogrel Treated Subjects Taking Aspirin and Having Stable Coronary Artery...
Characterization of the Pharmacokinetics (PK) Cmax of the Active Metabolite of Prasugrel and the Active Metabolite of ... Assessment of P2Y12 Reaction Units (PRU) by Treatment and Smoking Status [ Time Frame: Day 10 for Active Treatment Periods 1 ... Purinergic P2Y Receptor Antagonists. Purinergic P2 Receptor Antagonists. Purinergic Antagonists. To Top ... Blood samples for determination of plasma concentrations of the prasugrel active metabolite, clopidogrel active metabolite, and ...https://clinicaltrials.gov/ct2/show/NCT01260584
Pharmaceutical Compositions Comprising Prasugrel and Cyclodextrin Derivatives and Methods of Making and Using the Same -...
... active metabolite that irreversibly inhibits platelet activation and aggregation mediated by the P2Y12-receptor. Once bound, a ... Released ADP promotes platelet activation via the G-protein linked P2Y1 and P2Y12 purinergic receptors leading to further ... While the active metabolites of prasugrel and clopidogrel resulted in similar levels of platelet inhibition in vitro, the ... to its active metabolite compared to a clopidogrel loading dose of 300 mg.  Compositions comprising clopidogrel and a ...http://www.patentsencyclopedia.com/app/20130012534
Platelet Function Tests: Why They Fail to Guide Personalized Antithrombotic Medication | Journal of the American Heart...
Blockade of purinergic P2Y12 receptor greatly increases the platelet inhibitory actions of nitric oxide. Proc Natl Acad Sci USA ... Is there really a relationship between the plasma concentration of the active metabolite of clopidogrel and the results of ... The P2Y12 receptor antagonist prasugrel metabolite has been shown to inhibit neutrophil activation through a mechanism that ... P2Y12 receptors were shown to be important in early atheroma formation, and the latter was not inhibited by platelet P2Y12 ...http://jaha.ahajournals.org/content/4/5/e002094.full
Advantages of Fast-Acting ADP Receptor Blockade in Ischemic Heart Disease | Arteriosclerosis, Thrombosis, and Vascular Biology
However, they require metabolism in the liver and plasma levels of the active metabolite can vary between subjects, a small ... The C6-2B glioma cell P2YAC receptor is pharmacologically and molecularly identical to the platelet P2Y12 receptor. Br J ... Defective platelet aggregation and increased resistance to thrombosis in purinergic P2Y1 receptor-null mice. J Clin Invest. ... P2Y12, a new platelet ADP receptor, target of clopidogrel. Biochem Biophys Res Commun. 2001; 283: 379-383. ...http://atvb.ahajournals.org/content/23/2/158
Most recent papers with the keyword Biological Sciences | Read by QxMD
After an introduction to the purinergic receptor biology, this review summarizes current knowledge on P2Y12 receptor inhibitors ... Today, more than 60 years after the seminal work of R. A. Marcus, charge transfer is still a very active field of research. An ... In-cell NMR: from metabolites to macromolecules.. G Lippens, E Cahoreau, P Millard, C Charlier, J Lopez, X Hanoulle, J C ... P2Y12 inhibitors are a critical component of dual antiplatelet therapy (DAPT) - a combination of a P2Y12 receptor inhibitor and ...https://www.readbyqxmd.com/keyword/117410
Most recent papers with the keyword Mass spectrometry | Read by QxMD
... purinergic receptors and is a receptor for adenosine diphosphate (ADP). The P2Y12 receptor is involved in platelet aggregation ... Bioanalysis of a panel of neurotransmitters and their metabolites in plasma samples obtained from pediatric patients with ... Tripterygium wilfordii (TW) and the representative active component triptolide show positive therapeutic effect on the ... CLO is one such drug that specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor... ...https://www.readbyqxmd.com/keyword/10931
Bidirectional Microglia-Neuron Communication in the Healthy Brain
P2Y12) receptors on microglia that act in concert (magnification in center). (4) Purinergic activation leads to microglial ... these metabolites are released into the extracellular space at concentrations that could activate the respective receptor(s), ... the authors reported that microglial processes made preferential contact with more active neurons as measured by calcium flux ... A second adenosine receptor, the A2a receptor, has also been implicated in microglial process dynamics, and A2a receptor ...https://www.hindawi.com/journals/np/2013/456857/
Cangrelor - DrugBank
... who have not been yet treated by oral P2Y12 inhibitors. An advantage Cangrelor provides over oral P2Y12 inhibitors (such as ... prasugrel, ticagrelor, and clopidogrel) is that it is an active drug not requiring metabolic conversion therefore providing a ... reversible P2Y12 inhibitor for patients undergoing percutaneous coronary intervention (PCI) ... Purinergic Agents. *Purinergic Antagonists. *Purinergic P2 Receptor Antagonists. *Purinergic P2Y Receptor Antagonists ...https://www.drugbank.ca/drugs/DB06441
T Helper Cell Function and Extracellular ATP | BrainImmune: Trends in Neuroendocrine Immunology
Purinergic receptors in human placenta: evidence for functionally active P2X4, P2X7, P2Y2, and P2Y6. Am J Physiol Regul Integr ... Evidence that the purinergic receptor P2Y12 potentiates platelet shape change by a Rho kinase-dependent mechanism. Platelets ... from the complex interplay of several purinergic receptors simultaneously triggered by extracellular ATP and its metabolites. ... Purinergic receptors. P2 receptors are a class of plasma membrane receptors expressed by virtually all cell types. Their ...http://www.brainimmune.com/regulation-of-t-helper-cell-function-by-extracellular-atp/
Dual Anticoagulant and Antiplatelet Therapy for Coronary Artery Disease and Peripheral Artery Disease Patients |...
Roles of purinergic receptor P2Y, G protein-coupled 12 in the development of atherosclerosis in apolipoprotein E-deficient mice ... resulting in a broad variation in concentrations of the active metabolite. Recently, the IGNITE study (Implementing Gennomics ... The more potent P2Y12 blocker prasugrel was superior to clopidogrel in reducing the combined end point of vascular death, MI, ... Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity ...http://atvb.ahajournals.org/content/38/4/726
Multiple Electrode Aggregometry & Clopidogrel Resistance - Full Text View - ClinicalTrials.gov
Purinergic P2Y Receptor Antagonists. Purinergic P2 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. ... but their platelets respond normally to active metabolite added ex vivo. J Am Coll Cardiol. 2008 Dec 9;52(24):1968-77. doi: ... the first reversible oral P2Y(12) receptor antagonist, with clopidogrel in patients with acute coronary syndromes: Rationale, ... with poor responsiveness to thienopyridine treatment or with diabetes have lower levels of circulating active metabolite, ...https://clinicaltrials.gov/ct2/show/NCT01991093?term=%22Coronary+Artery+Disease%22&lup_s=08%2F07%2F2014&lup_d=14&show_rss=Y&sel_rss=mod14
Diabetes mellitus and platelet reactivity in patients under prasugrel or ticagrelor treatment: an observational study |...
Antiplatelet agentsAntiplatelet drugsDiabetes mellitusInsulinP2Y12 purinergic receptors. Background. Patients with type 2 ... Moreover, and concerning the other thienopyridine, clopidogrel, active metabolite kinetic profile-and to a lesser degree ... Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc Ther. 2009;27:259-74.PubMed CentralPubMed ... Moreover, ticagrelor is a reversible P2Y12 ADP receptor blocker, administered twice daily, which may be more optimal for ...https://cardiab.biomedcentral.com/articles/10.1186/s12933-015-0232-1
Frontiers | Purinergic Signaling in Mast Cell Degranulation and Asthma | Pharmacology
However, recent evidence showed that many other receptors, such as G protein-coupled receptors and ligand-gated ion channels, ... However, recent evidence showed that many other receptors, such as G protein-coupled receptors and ligand-gated ion channels, ... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ...https://www.frontiersin.org/articles/10.3389/fphar.2017.00947/full
New aspects on efficient anticoagulation and antiplatelet strategies in sheep | BMC Veterinary Research | Full Text
... while clopidogrel and its metabolite carboxylic acid were detected in every plasma sample. High dose ticagrelor (375 mg bid) ... Gachet C: P2Y(12) receptors in platelets and other hematopoietic and non-hematopoietic cells. Purinergic Signal. 2012, 8 (3): ... or an accelerated clearance of the active metabolite, or the above-mentioned genetic variations concerning the cytochrome P450 ... Clopidogrel is an oral ADP receptor antagonist which inhibits platelet activation through blockade of the P2Y12 ADP receptor on ...https://0-bmcvetres-biomedcentral-com.brum.beds.ac.uk/articles/10.1186/1746-6148-9-192