arginyl-glycyl-aspartyl-valine and Disease-Models--Animal

In this study, a new class of phenolic tetrahydro-beta-carboline RGD peptidomimetic conjugates was designed and synthesized. The radical scavenging activities of these newly synthesized compounds 12a-c were evaluated in PC12 cell survival assays. The NO scavenging activities of these compounds were confirmed in the acetylcholine-induced vasorelaxation assay. Compounds 12a-c were efficacious in a rat arterial thrombosis model, and were active in ADP- or PAF-induced in vitro platelet aggregation assays, which suggests these compounds also possess anti-thrombotic activity. The beneficial effects of dual-acting agent 12c were demonstrated on the ischemia-reperfusion induced cardiac infarct size and oxidative change in an in vivo rat model.

Topics: Animals; Carbolines; Cell Survival; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Design; Fibrinolytic Agents; Free Radical Scavengers; Molecular Structure; Oligopeptides; PC12 Cells; Phenol; Platelet Aggregation; Platelet Aggregation Inhibitors; Rats; Thrombosis