Structure
Tezosentan is a selective endothelin receptor antagonist with a quinazoline core linked to aromatic substituents and amine groups.
Chemical Formula: C₂₄H₂₂N₄O₆S₂
Mode of Action
Selective Endothelin Receptor Blocking: Primarily antagonizes ETA receptors, reducing vasoconstriction and vascular remodeling.
Vasodilation: Decreases systemic and pulmonary vascular resistance by inhibiting ET-1-mediated vasoconstriction.
Anti-Proliferative Effects: Prevents endothelial cell proliferation and fibrosis associated with chronic hypertension.
Uses of Tezosentan
Pulmonary Arterial Hypertension (PAH): Enhances exercise capacity and reduces pulmonary vascular resistance.
Heart Failure: Investigated for its potential in managing heart failure by reducing afterload.
Stroke: Explored for neuroprotective effects by improving cerebral blood flow and reducing vasospasm.