Thrombin receptor antagonists

TL;DR: In this article, compositions for treating IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudoobstruction), and disorders associated with constipation, e.g. constipation associated with use of opiate pain killers, post

TL;DR: This study characterizes the biochemical and pharmacological actions of pyrroloquinazoline inhibitors of protease activated receptor-1 (PAR-1) in human platelets and coronary artery smooth muscle cells (hCASMC) and demonstrates that SCH 79797 and SCH 203099 are potent, selective antagonists of PAR-1 in human Platelets and hCAS MC.

TL;DR: TRA*CER will define efficacy and safety of the novel platelet PAR-1 inhibitor SCH 530348 in the treatment of high-risk patients with NSTE ACS in the setting of current treatment strategies.

TL;DR: The present paper as mentioned in this paper provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses, and further provides a combination of pharmacologically active agents and a pharmaceutical composition.

TL;DR: Section 1 - General Aspects of Medicinal Chemistry Section 2 - Lead Compound Discovery Strategies Section 3 - Primary Exploration of Structure-Activity Relationships Section 4 - Substituents and Functions: Qualitative and Quantitative aspects of structure- activity Relationships.

TL;DR: Four PARs have now been identified and cells have evolved a trafficking solution to the signaling problem presented by PARs, which is critical for termination of thrombin signaling.

TL;DR: This review summarizes current knowledge about the in vitro pharmacological properties of important CB1 and CB2 receptor ligands and pays particular attention to the binding properties of these ligands, to the efficacies of cannabinoid receptor agonists, as determined using cyclic AMP or [35S]GTPgammaS binding assays, and to selected examples of how these pharmacological Properties can be influenced by chemical structure.

TL;DR: While most studies of thrombin have concentrated on its action on cells involved in blood clotting and wound healing, it is now becoming apparent that it can modulate the growth and differentiation status of cells of neuronal origin.