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As seen in human platelets, PAR1 and PAR4 are the functional thrombin receptors, whereas PAR3 and PAR4 are functional thrombin receptors in mouse platelets Thrombin receptors are also differentially expressed in cell types, e.g. PAR1 is expressed in fibroblasts, smooth muscle cells, sensory neurons and glial cells, whereas the other two are ...
Platelets secrete thromboxane A2, which acts on the platelet's own thromboxane receptors on the platelet surface (hence the so-called "out-in" mechanism), and those of other platelets. These receptors trigger intraplatelet signaling, which converts GPIIb/IIIa receptors to their active form to initiate aggregation .
Adenosine diphosphate (ADP) is a platelet agonist. When it is added to saline-diluted whole blood in the test cuvette, it stimulates the ADP receptors on platelets, activating the platelets. The activation of the platelets leads to shape change and degranulation, and the released content of the granules further activates the platelets.
TP(-/-) mice are: a) resistant to the cardiogenic shock caused by infusion of the TP agonist, U46619, or the prostaglandin and thromboxane A 2 precursor, arachidonic acid; b) partially protected from the cardiac damage caused by hypertension in IP-receptor deficient mice feed a high salt diet; c) prevented from developing angiotensin II-induced ...
It is believed that the vasoconstriction caused by thromboxanes plays a role in Prinzmetal's angina. Omega-3 fatty acids are metabolized to produce higher levels of TxA 3, which is relatively less potent than TxA 2 and PGI 3; therefore, there is a balance shift toward inhibition of vasoconstriction and platelet aggregation. It is believed that ...
Receptors that mediate TXA 2 actions are thromboxane A 2 receptors. The human TXA 2 receptor (TP) is a typical G protein-coupled receptor (GPCR) with seven transmembrane segments. In humans, two TP receptor splice variants – TPα and TPβ – have so far been cloned.
Protease-activated receptors (PAR) are a subfamily of related G protein-coupled receptors that are activated by cleavage of part of their extracellular domain. They are highly expressed in platelets , and also on endothelial cells , fibroblasts, immune cells, myocytes , neurons , and tissues that line the gastrointestinal tract.
Vasopressin receptor antagonists (VRAs) are drugs that block vasopressin receptors. Most commonly VRAs are used to treat hyponatremia caused by syndrome of inappropriate antidiuretic hormone secretion (SIADH), congestive heart failure (CHF) and cirrhosis. [2] Somatostatin is a competitive inhibitor. [5]