Use of [3H]trimetoquinol as a radioligand in human platelets: interaction with putative endoperoxide/thromboxane A2 receptor sites.

  title={Use of [3H]trimetoquinol as a radioligand in human platelets: interaction with putative endoperoxide/thromboxane A2 receptor sites.},
  author={Chang Ho Ahn and Lane J. Wallace and D. D. Miller and Dennis R. Feller},
  journal={Thrombosis research},
  volume={50 3},
Pharmacologic antagonism of thromboxane A2 receptors by trimetoquinol analogs in vitro and in vivo.
In vivo antithrombotic potencies of these compounds were consistent with the in vitro potencies as TXA2 receptor antagonists in platelet systems and protected animals against death.
Prostanoid receptor antagonists: development strategies and therapeutic applications
This review is intended to provide overviews of each antagonist class (including prostamide antagonists), covering major development strategies and current and potential clinical usage.
International Union of Basic and Clinical Pharmacology. LXXXIII: Classification of Prostanoid Receptors, Updating 15 Years of Progress
The DP2 receptor, also termed CRTH2, has little structural resemblance to DP1 and other receptors described in the original prostanoid receptor classification and is anticipated to lead to novel therapeutic entities.


Identification of a putative thromboxane A2/prostaglandin H2 receptor in human platelet membranes.
The binding of the competitive thromboxane A2/prostaglandin H2 (TXA2/PGH2) antagonist and [125I]PTA-OH to membranes prepared from human platelets was characterized, consistent with the notion that this binding site may represent the platelet TXA-OH receptor.
Effect of trimetoquinol analogs for antagonism of endoperoxide/thromboxane A2-mediated responses in human platelets and rat aorta.
It is concluded that selectivity for these two pharmacological properties of TMQ can be achieved by appropriate stereochemical modification of the tetrahydroisoquinoline nucleus.
Ligand binding to thromboxane receptors on human platelets: correlation with biological activity
1 The preparation of enantiomerically pure [3H]‐15 (S) 9, 11‐epoxymethano PGH2 (a thromboxane A2‐like agonist) has enabled the binding of ligands to the thromboxane receptor of the human platelet to
Synthesis and platelet antiaggregatory activity of trimetoquinol analogs as endoperoxide/thromboxane A2 antagonists.
Results suggest that the putative sites of interaction for the trimethoxy ring system of TMQ in platelet systems will tolerate large, lipid soluble groups but will not tolerate large changes in the electronic characteristics of the ring system.
Thromboxanes: a new group of biologically active compounds derived from prostaglandin endoperoxides.
Evidence is presented that the more unstable and major component of rabbit aorta contracting substance (RCS) formed in platelets and guinea pig lung is also thromboxane A2.