Antagonist für P2Y12-Purinozeptor; hemmt die ADP-induzierte Aggregation in Ratten-Thrombozyten und antagonisiert die ADP-induzierte Hemmung von cAMP in Thrombozyten der Ratte und des Menschen in Gegenwart von PGE1, ohne die P2Y1-Rezeptor-induzierte PLC-Aktivität in transfizierten Astrozytomzellen zu beeinflussen.
British journal of pharmacology, 151(1), 73-81 (2007-03-14)
This study analysed the contribution of the purinergic system to enteric neurotransmission in the longitudinal muscle of mouse distal colon. Motor responses to exogenous ATP and to nerve stimulation in vitro were assessed as changes in isometric tension. ATP induced
Journal of medicinal chemistry, 45(26), 5694-5709 (2002-12-13)
Activation by ADP of both P2Y(1) and P2Y(12) receptors in platelets contributes to platelet aggregation, and antagonists at these receptor subtypes have antithrombotic properties. In an earlier publication, we have characterized the SAR as P2Y(1) receptor antagonists of acyclic analogues
The Journal of allergy and clinical immunology, 125(2), 477-482 (2010-02-18)
Cysteinyl leukotrienes (cysLTs) are recognized to act via receptors (cysLTRs) expressed on cell surface plasma membranes. Agents that block cysLT(1) receptor (cysLT(1)R) are therapeutics for allergic disorders. Eosinophils contain multiple preformed proteins stored within their intracellular granules. Cell-free eosinophil granules
It is known that adenosine 5'-triphosphate (ATP) is released along with the neurotransmitter acetylcholine (ACh) from motor nerve terminals. At mammalian neuromuscular junctions (NMJs), we have previously demonstrated that ATP is able to decrease ACh secretion by activation of P2Y
The release of ADP from platelet dense granules and its binding to platelet P2Y12 receptors is key to amplifying the initial hemostatic response and propagating thrombus formation. P2Y12 has thus emerged as a therapeutic target to safely and effectively prevent
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