Tezosentan is an endothelin receptor antagonist used in heart failure to improve blood flow and reduce vascular resistance.
Structure of Tezosentan
- 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 remodelling.
- 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.
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Uses
- 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.
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