• Our outcomes reveal the antiplatelet aggregation properties of Alibertia edulis leaf extract, rutin and caffeic acid offering pharmacological details about its origin from cyclooxygenase 1 inhibition and its downstream pathway. (lindenbachlab.org)
  • Over the past decade, antithrombotic effects of aspirin due to inhibition of cyclooxygenase activity in platelets and subsequent reduction in thromboxane A2 synthesis have been explored for the treatment and prevention of recurrence of myocardial infarction, angina and cerebral infarction. (ijpsonline.com)
  • Nicotine limits the release of prostacyclin synthesis through the inhibition of cyclooxygenase. (rnspeak.com)
  • Pharmacological inhibition of thromboxane-synthetase and platelet aggregation: Modulatory role of cyclooxygenase products. (unimib.it)
  • Biochemical evidence includes an imbalance in the prostacyclin:thromboxane ratio and high circulating concentrations of von Willebrand factor, endothelin, and cellular fibronectin. (health.am)
  • Tromboxane synthetase inhibition results in increased platelet sensivity to prostacyclin. (unimib.it)
  • Effect of thromboxane A2 inhibition and antagonism on prostaglandin and leukotriene synthesis in glomerular immune injury. (mcw.edu)
  • Localization of authentic thromboxane A2/prostaglandin H2 receptor in the rat kidney. (mcw.edu)
  • however, higher doses of aspirin are required to attain further inhibition. (wikipedia.org)
  • The test results were reported as aspirin-reaction unit (ARU) for aspirin and P2Y 12 reaction units (PRU), baseline (BASE), and percentage inhibition for the P2Y 12 assay and were summarized as mean ± SD of the values. (ajnr.org)
  • Aspirin resistance", defined as an inadequate suppression of platelet thromboxane production or an inadequate inhibition of platelet aggregation in vitro from low-dose aspirin, has been linked to a several-fold increased risk of recurrent atherothrombotic events among patients at high risk. (escardio.org)
  • Failure of aspirin to suppress platelet thromboxane production or to inhibit platelet aggregation in vitro has been convincingly linked to an inadequate protection against atherothrombotic events. (escardio.org)
  • The most important cardiovascular effect of aspirin is mediated by irreversible inhibition of platelet cyclooxigenase-1 (COX-1) resulting in the suppression of thromboxane (TX) A2 production. (escardio.org)
  • Aspirin, which exerts its antiplatelet effects by inhibiting thromboxane A2 production, has been the mainstay of antiplatelet therapy in patients with ACS. (jabfm.org)
  • The limited anti-thrombotic efficacy of aspirin may reflect the fact that it blocks only one source of ADP which is that released in a thromboxane-dependent manner following platelet adhesion (see e.g. (justia.com)
  • Aspirin-resistant thromboxane biosynthesis and the risk of myocardial infarction, stroke, or cardiovascular death in patients at high risk for cardiovascular events. (jscientia.org)
  • Aspirin does not modify the Clop1dogrel mediated inhibition of ADP-induced platelet aggregation. (sandarmyaingmyanmar.com)
  • Thromboxane inhibitors are broadly classified as either those that inhibit the synthesis of thromboxane, or those that inhibit the target effect of it. (wikipedia.org)
  • Thromboxane synthase inhibitors inhibit the final enzyme (thromboxane synthase) in the synthesis of thromboxane. (wikipedia.org)
  • Thromboxane is named for its role in blood clot formation (thrombosis). (wikipedia.org)
  • Platelet inhibition is a prerequisite for the prevention of acute or subacute thrombosis in various neurointerventional procedures such as stent placement in atherosclerotic lesions or stent-assisted coiling of aneurysms. (ajnr.org)
  • Ifetroban is a potent and selective thromboxane receptor antagonist. (wikipedia.org)
  • It also stimulates the release of the potent vasoconstrictor thromboxane A 2 . (rnspeak.com)
  • Steady state concentrations of CV6504 and thromboxane B2 (an indirect measure of thromboxane A2 synthetase (TA2S) inhibition) were made. (ox.ac.uk)
  • Picotamide has activity both as a thromboxane synthase inhibitor and as a thromboxane receptor antagonist. (wikipedia.org)
  • Arachidonic acid elevated ranges of calcium and thromboxane B2, phosphorylation of vasodilator-stimulated phosphoprotein Ser157 and Ser239, and protein kinase Cβ, which have been considerably decreased by Alibertia edulis leaf extract, rutin, and caffeic acid as effectively mixtures of rutin/caffeic acid. (lindenbachlab.org)
  • therefore, there is a balance shift toward inhibition of vasoconstriction and platelet aggregation. (wikipedia.org)
  • Most of the developments in pharmacotherapy have been in targeting platelet inhibition because platelet aggregation and the resultant formation of platelet-rich thrombi are the primary events in the pathogenesis of ACS. (jabfm.org)
  • It has now been found that certain compounds within the scope of International Patent Application WO 9905143 but not specifically disclosed therein exhibit high potency combined with surprisingly high metabolic stability and bioavailibility, such that the predicted therapeutic dose for prolonged inhibition of aggregation in man shows advantage. (justia.com)
  • The inhibitory effects of α-tocopherol on platelet function in vivo and ex vivo have been well established [ 14 - 18 ], but inhibition of platelet aggregation by α-tocopherol in vitro requires non-physiologically high levels of α-tocopherol [ 14 ]. (biomedcentral.com)
  • PAR4 Thr120 induces greater signaling and is associated with greater platelet aggregation and reduced inhibition by a PAR4 antagonist. (ashpublications.org)
  • Conclusions: GF109203X and Go6983 inhibit neurogenic, alpha(1)-adrenergic, and thromboxane A(2)-induced smooth muscle contractions in the human prostate, suggesting a role of PKC for human prostate smooth muscle contraction. (uni-muenchen.de)
  • Changes in glomerular thromboxane A2 receptor expression and ligand binding following immune injury. (mcw.edu)
  • In addition, they had enhanced excretion of thromboxane (a vasoconstrictor). (medscape.com)
  • The inhibitors of the target effects of thromboxane are the thromboxane receptor antagonist, including terutroban. (wikipedia.org)
  • The eicosanoid family encompasses thromboxanes, prostacyclins, leukotrienes, hydroxyeicosatetraenoic acids (HETEs), epoxyeicosatrienic acids (EETs), lipoxins, and isoprostanes, the last of which can be generated by nonenzymatic oxidative mechanisms and may serve as markers of oxidative stress in humans. (jci.org)
  • However, the inhibition of eicosanoid generation and lipid peroxidation by the fixed oil of N. sativa is greater than is expected from its content of thymoquinone (ca. 0.2% w/v), and it is possible that other components such as the unusual C20:2 unsaturated fatty acids may contribute also to its anti-eicosanoid and antioxidant activity. (thieme-connect.com)
  • The crude fixed oil and pure thymoquinone both inhibited the cyclo-oxygenase and 5-lipoxygenase pathways of arachidonate metabolism in rat peritoneal leukocytes stimulated with calcium ionophore A23187, as shown by dose-dependent inhibition of thromboxane B 2 and leukotriene B 4 , respectively. (thieme-connect.com)
  • Contractions were induced by electric field stimulation (EFS), alpha(1)-adrenergic agonists (noradrenaline, phenylephrine, methoxamine), thromboxane A(2) analog U46619, endothelin-1, or calcium chloride in an organ bath. (uni-muenchen.de)
  • The inhibition may by be imparted by inhibition of calcium sensitivity. (uni-muenchen.de)
  • Leukotriene B4, thromboxane B2, and inflammatory products also have been discovered within herniated human disks after surgery. (medscape.com)
  • Suffusion of the muscle with U46619 (1-100 nM), a thromboxane A2 mimetic, led to a significantly greater vasoconstriction in exposed animals compared to control (max % of control -22 +/- 3.4% sham, -31 +/- 4.0% exposed). (cdc.gov)
  • secondary objectives included estimation of pharmacokinetics of CV6504, target-enzyme inhibition, safety and tolerance, quality of life and survival. (ox.ac.uk)
  • Thromboxane acts by binding to any of the thromboxane receptors, G-protein-coupled receptors coupled to the G protein Gq. (wikipedia.org)
  • The radicular LBP caused by spinal stenosis is probably related to the inhibition of normal nerve root vascular flow with resultant nerve root nutrition, nerve root edema, and nerve root dysfunction. (medscape.com)
  • People with asthma tend to have increased thromboxane production, and analogs of thromboxane act as bronchoconstrictors in patients with asthma. (wikipedia.org)
  • Ces résultats semblent indiquer que l'utilisation de l'alun en tant qu'antiplaquettaire oral pourrait faire l'objet d'études complémentaires, en tenant compte des effets secondaires éventuels notamment chez les patients dont la fonction rénale est altérée. (who.int)
  • The effects include mitochondrial swelling and inhibition of respiratory function and energy (adenosine triphosphate) production. (medscape.com)
  • The mainstay of ACS treatment revolves around platelet inhibition. (jabfm.org)
  • Cytokine inhibition preserves renal hemodynamic function following mesangial cell immune injury. (mcw.edu)