Bosentan is an endothelin receptor antagonist used to treat pulmonary arterial hypertension by relaxing blood vessels.
Structure of Bosentan
- Bosentan is a non-selective endothelin receptor antagonist with a central benzothiazole core linked to aromatic rings and amine groups.
- Chemical Formula: C₂₀H₂₀N₂O₂S₂
Mode of Action
- Endothelin Receptor Blocking: Antagonizes endothelin-1 (ET-1) receptors (ETA and ETB), preventing vasoconstriction.
- Vasodilation: Promotes relaxation of vascular smooth muscle, reducing pulmonary vascular resistance.
- Anti-Proliferative Effects: Inhibits vascular smooth muscle cell proliferation and fibrosis.
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Uses
- Pulmonary Arterial Hypertension (PAH): Reduces pulmonary arterial pressure and improves exercise capacity.
- Systemic Sclerosis-Associated PAH: Manages pulmonary hypertension in patients with systemic sclerosis.
- Diabetic Nephropathy: Investigated for its role in reducing renal fibrosis and proteinuria.
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