Biomaterial Database

Binding of a thromboxane A2/prostaglandin H2 agonist [3H]U46619 to washed human platelets. 1987

N Liel, and D E Mais, and P V Halushka

Department of Cell and Molecular Pharmacology and Therapeutics, Medical University of South Carolina, Charleston 29425.

The binding characteristics of [3H]U46619 to washed human platelets were studied. [3H]U46619 binding to washed human platelets was saturable and displaceable. Kinetic studies yielded a Kd of 11 +/- 4 nM (n = 4). Scatchard analysis of equilibrium binding studies revealed one class of high affinity binding sites with a Kd of 20 +/- 7 nM and a Bmax of 9.1 +/- 2.3 fmole/10(7) platelets (550 +/- 141 binding sites per platelet) (n = 4). A number of compounds that act as either agonists or antagonists of the TXA2/PGH2 receptor were tested for their ability to inhibit the binding of [3H]U46619 to washed human platelets. The Kds of the agonists and antagonists were similar to their potencies to induce or inhibit platelet aggregation. These data provide some evidence that [3H]U46619 binds to the putative human platelet TXA2/PGH2 receptor.

UI	MeSH Term	Description	Entries
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D010974	Platelet Aggregation	The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.	Aggregation, Platelet
D011450	Prostaglandin Endoperoxides, Synthetic	Synthetic compounds that are analogs of the naturally occurring prostaglandin endoperoxides and that mimic their pharmacologic and physiologic activities. They are usually more stable than the naturally occurring compounds.	Prostaglandin Endoperoxide Analogs,Prostaglandin Endoperoxide Analogues,Synthetic Prostaglandin Endoperoxides,Analogues, Prostaglandin Endoperoxide,Endoperoxide Analogues, Prostaglandin,Endoperoxides, Synthetic Prostaglandin
D011982	Receptors, Prostaglandin	Cell surface receptors that bind prostaglandins with high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin receptor subtypes have been tentatively named according to their relative affinities for the endogenous prostaglandins. They include those which prefer prostaglandin D2 (DP receptors), prostaglandin E2 (EP1, EP2, and EP3 receptors), prostaglandin F2-alpha (FP receptors), and prostacyclin (IP receptors).	Prostaglandin Receptors,Prostaglandin Receptor,Receptor, Prostaglandin,Receptors, Prostaglandins,Prostaglandins Receptors
D001792	Blood Platelets	Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation.	Platelets,Thrombocytes,Blood Platelet,Platelet,Platelet, Blood,Platelets, Blood,Thrombocyte
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001667	Binding, Competitive	The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.	Competitive Binding
D017482	Receptors, Thromboxane	Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.	TP Receptors,Thromboxane Receptors,Receptors, Thromboxanes,TP Receptor,Thromboxane Receptor,Receptor, TP,Receptor, Thromboxane,Receptors, TP,Thromboxanes Receptors
D044244	Receptors, Thromboxane A2, Prostaglandin H2	A subclass of eicosanoid receptors that have specificity for THROMBOXANE A2 and PROSTAGLANDIN H2.	Prostaglandin H2 Receptor,Receptors, Prostaglandin H2,Receptors, TXA2-PGH2,Receptors, Thromboxane A2,TXA2-PGH2 Receptors,Thromboxane A2, Prostaglandin H2 Receptors,PGH2 Receptors,Thromboxane A2 Receptor,H2 Receptors, Prostaglandin,Prostaglandin H2 Receptors,Receptor, Prostaglandin H2,Receptors, PGH2,Receptors, TXA2 PGH2,TXA2 PGH2 Receptors
D019796	15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid	A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)	(15S)-Hydroxy-11 alpha, 9 alpha-(epoxymethano)prosta-5Z, 13E-dienoic Acid,(15S)hydroxy-9alpha,11alpha-(epoxymethano)prosta-5,13-dienoic acid,11 alpha,9 alpha-Epoxymethano PGH2,9,11-Dideoxy-11 alpha,9 alpha-epoxymethanoprostaglandin F2 alpha,9,11-Dideoxy-11 alpha,9-alpha-epoxymethano-PGF2 alpha,9,11-epoxymethano-PGH2,U-44619,U-46619,U44619,U46619,11 alpha,9 alpha Epoxymethano PGH2,9,11 epoxymethano PGH2,U 44619,U 46619