Results 181 to 190 of about 563,890 (226)

Receptors for thromboxane and prostaglandins

1984
The elucidation of the structures of thomboxane A2 and prostaglandin D2, E2, F2a and I2, all products of the cyclic endoperoxides PGG2/PGH2, was accompanied by the demonstration of a distinctive biological profile for each compound. Stimulant or inhibitory activity was often observed at nanomolar concentrations.
R. L. Jones, N. H. Wilson, R. A. Armstrong, Y. J. Dong   +3 more
openaire   +1 more source

A New Family of Thromboxane Receptor Antagonists with Secondary Thromboxane Synthase Inhibition

The Journal of Pharmacology and Experimental Therapeutics, 2002
We report herein a novel class of thromboxane receptor (TP receptor) antagonists modeled on unstable natural lipids that we identified several years ago, the hepoxilins. These antagonists have been rendered chemically and biologically more stable than the natural compounds through structural modification by chemical synthesis.
Cecil R, Pace-Asciak, Denis, Reynaud, Peter, Demin, Rukshana, Aslam, Andrea, Sun   +4 more
openaire   +2 more sources

Pharmacological Evidence for Thromboxane Receptor Heterogeneity—Implications for the Eye

Journal of Ocular Pharmacology and Therapeutics, 1997
The pharmacological activity of two novel thromboxane A2 (TxA2)-mimetics, AGN191976 and AGN192093, was investigated in vitro, using standard organ bath assays and human platelets, to determine potency and selectivity at various prostanoid (PG-) receptors.
Krauss, Achim H.-P., Woodward, David F., Burk, Robert M., Gac, Todd S., Gibson, Linda L., Protzman, C.E., Abbass, F., Marshall, K.; id_orcid 0000-0003-0140-7550, Senior, J.   +8 more
openaire   +4 more sources

The Thromboxane/Endoperoxide Receptor (TP): The Common Villain

Journal of Cardiovascular Pharmacology, 2010
The stimulation of thromboxane/endoperoxide receptors (TP) elicits diverse physiological/pathophysiological reactions, including platelet aggregation and contraction of vascular smooth muscle. Furthermore, the activation of endothelial TP promotes the expression of adhesion molecules and favors adhesion and infiltration of monocytes/macrophages.
Feletou, M, Verbeuren, TJ, Vanhoutte, PM
openaire   +3 more sources

Characterization of Thromboxane Receptors in Human Platelets

1985
This chapter deals with the characterization of the human platelet thromboxane receptor in terms of its interaction with natural and synthetic prostanoids. Accurate information of this type will enable comparisons to be made with thromboxane receptors in platelets from other species and in other tissues, for example, vascular smooth muscle.
R L, Jones, N H, Wilson, R A, Armstrong
openaire   +2 more sources

Alterations in Thromboxane Synthase and Thromboxane A2 Receptors in Experimental Alcoholic Liver Disease

The Journal of Pharmacology and Experimental Therapeutics, 1997
We have previously shown that hepatic thromboxane production is increased in experimental alcoholic liver disease. The present study was designed to investigate the cell type in liver responsible for increased thromboxane synthesis and the role of the thromboxane receptor system in the pathogenesis of liver injury.
A A, Nanji, A, Rahemtulla, L, Maio, S, Khwaja, S, Zhao, S R, Tahan, P, Thomas   +6 more
openaire   +2 more sources

Thromboxane synthesis inhibitors and receptor antagonists

Thrombosis Research, 1990
The biochemical, functional and clinical consequences of thromboxane (TX) A2 synthesis inhibition and receptor antagonism are reviewed, with emphasis on human studies in health and disease. Both platelet and glomerular TXA2 synthesis and action are discussed as potential targets for cyclooxygenase inhibitors, TX-synthase inhibitors and TXA2-receptor ...
openaire   +2 more sources

Terbogrel, a dual-acting agent for thromboxane receptor antagonism and thromboxane synthase inhibition

Acta Crystallographica Section C Crystal Structure Communications, 2000
Terbogrel, (E)-6-[4-(3-tert-butyl-2-cyanoguanidino)phenyl]-6-(3-pyridyl)hex-5 -enoic acid, C(23)H(27)N(5)O(2), a mixed thromboxane A(2) receptor antagonist and thromboxane A(2) synthase inhibitor, shows a hairpin-like conformation stabilized by an intramolecular hydrogen bond.
Michaux, Catherine, Norberg, Bernadette, Dogné, Jean-Michel, Durant, François, Masereel, Bernard, Delarge, Jacques, Wouters, Johan   +6 more
openaire   +3 more sources

Thromboxane synthetase inhibitors differentially antagonize thromboxane receptors in vascular smooth muscle

Naunyn-Schmiedeberg's Archives of Pharmacology, 1981
A number of thromboxane (Tx) synthetase inhibitors have been found to prevent thromboxane release in acute cardiopulmonary disorders. However, little is known about Tx receptor antagonism by these substances. Imidazole, UK-37,248 and pinane thromboxane A2 (PTA2) were tested in isolated perfused cat coronary arteries, spirally cut rabbit pulmonary ...
E F, Smith, A M, Lefer, J B, Smith, K C, Nicolaou   +3 more
openaire   +2 more sources

Effect of Receptor Number on Desensitization of the Mouse Thromboxane Receptor

Biochemical Pharmacology, 1998
Desensitization of G-protein coupled receptors limits the physiologic effects of an agonist. Short-term desensitization mechanisms are critically dependent on receptor phosphorylation by protein kinases. The effectiveness of these regulatory mechanisms might be limited by substrate (receptor) availability.
openaire   +2 more sources