This study evaluated the effects of two PAR1 antagonists on vessels contracted by SFLLR. ER 121958 antagonized the SFLLR-induced contraction on rat denuded superior mesenteric artery and pig corona...
AbstractThe synthesis of a designed, sterically congested geminal dimethyl‐bearing PAR‐1 antagonist was achieved by a route of ten steps, with the oxidation of an electron‐rich benzaldehyde, the co...
Graphical abstractTwo series of new PAR1 antagonists have been identified. The first incorporates a cinnamoylpiperidine motif and the second a cinnamoylpyridine pattern. The synthesis, biological a...
Target id: 348 Nomenclature: PAR2 Family: Proteinase-activated receptors
The IUPHAR/BPS Guide to Pharmacology. PAR1 - Proteinase-activated receptors. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
Octahydroindene was identified as a novel scaffold for protease activated receptor 1 (PAR1) antagonists. Herein, the 2-position (C2) was explored for structure–activity relationship (SAR) studies. ...
Vorapaxar is an orally active protease-activated receptor 1 (PAR-1) antagonist that inhibits thrombin-induced platelet aggregation. This open-label study a
Here, we describe the development of a series of highly selective PAR4 antagonists with nanomolar potency and selectivity versus PAR1, derived from the indole-based 3. Of these, 9j (PAR4 IC50 = 445...
Summary. Background: Thrombin receptor antagonists blocking protease-activated receptor-1 (PAR-1) on platelets represent a new class of oral antiplatelet agents for patients with atherothrombotic...
By applying a diversity oriented synthesis strategy for the search of new antagonists of the thrombin receptor PAR1, a series of peptide-based ureas and thioureas, including analogues of the PAR1 r...