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Bosentan

Structure

  • Bosentan is a non-selective endothelin receptor antagonist with a central benzothiazole core linked to aromatic rings and amine groups.

  • Chemical Formula: C₂₀H₂₀N₂O₂S₂

    Chemical Formula of Bosentan
Structure of Bosentan
Structure of Bosentan

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.

Uses of Bosentan

  • 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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