Novel therapeutic strategies for impaired endothelium-dependent vascular relaxation

Abstract

Impaired vascular relaxation is a common aetiology in many cardiovascular diseases and, in most cases, disequilibria in the amounts of endothelium-derived relaxing and constricting factors is the root of problem. Endothelium-derived vasoactive factors modulate vascular tone, smooth muscle cell proliferation, blood coagulation and fibrinolysis, lipoprotein metabolism and the interaction of platelet and leukocyte with the vascular wall. Although the synthesis and release of endothelium-derived vasoactive substances are vulnerable to pathogenic insults, endothelial dysfunction can be corrected pharmacologically using inhibitors of the renin–angiotensin system, endothelin antagonists, inductors of angiogenesis and other compounds. Many recent patents have provided novel formulations of drugs targeting dysfunctional endothelium. Optimised pharmacodynamic and pharmacokinetic properties of these drugs would greatly improve their clinical applications.

• angiogenesis
• angiotensin II
• angiotensin-converting enzyme
• cardiovascular diseases
• endothelial dysfunction
• endothelin