Binding kinetics and antiplatelet activities of picotamide, a thromboxane A2 receptor antagonist
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چکیده
منابع مشابه
Thromboxane A2 Synthase Inhibitor and Thromboxane A2/Prostaglandin Endoperoxide Receptor Antagonist, Versus Aspirin
Background Aspirin, by nonselectively blocking cyclooxygenase both in platelets and in endothelial cells, not only inhibits the thromboxane A2 pathway of platelet activation but at the same time also the generation of vasodilating and platelet-inhibitory prostanoids, such as prostacyclin, by the endothelial cells. Ridogrel, by inhibiting thromboxane A2 synthase and blocking the thromboxane A2/p...
متن کاملThe receptor antagonist picotamide inhibits adrenergic and thromboxane-induced contraction of hyperplastic human prostate smooth muscle.
Inhibition of prostate smooth muscle contraction is an important strategy for medical treatment of lower urinary tract symptoms (LUTS). Besides α1-adrenoceptors, prostate smooth muscle contraction is induced by activation of thromboxane (TXA2) receptors (TXA2-R). Here, we examined the effects of the TXA2-R antagonist picotamide on contraction of human prostate tissue. Prostate tissues were obta...
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BACKGROUND AND PURPOSE Arachidonate metabolites have been implicated in the development of cerebral injury after ischemia. Particular importance has been placed on the balance of thromboxane A2 and prostaglandin I2 because of its regulative activity on platelet functions and arterial tone. The purpose of the present study was to shed light on the role of thromboxane A2 in postischemic brain inj...
متن کاملTimosaponin AIII induces antiplatelet and antithrombotic activity via Gq-mediated signaling by the thromboxane A2 receptor
The thromboxane (Tx) A2 pathway is a major contributor to the amplification of initial platelet activation and is therefore a key drug target. To identify potent small-molecule inhibitors of the thromboxane prostaglandin (TP) receptor, we screened a small steroidal saponin library using U46619-induced rat platelet aggregation assays. Timosaponin AIII (TAIII) was identified as a potent inhibitor...
متن کاملDifferential effect of pH on thromboxane A2/prostaglandin H2 receptor agonist and antagonist binding in human platelets.
The effects of changes in pH on the binding of agonists and antagonists to the human platelet thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor were determined. Competition binding studies were performed with the TXA2/PGH2 mimetic [1S-1 alpha,2 beta (5Z), 3 alpha(1E,3R*),4 alpha)]-7-[3-(3-hydroxy-4'-iodophenoxy)-1-buteny) 7-oxabicyclo-[2.2.1]-heptan-2-yl]-5-heptenoic acid ([125I]BOP). The pH...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 1994
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.1994.tb13033.x