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Tezosentan

BP-S-5-MEDICINAL CHEMISTRY
1 min read

Structure

  • Tezosentan is a selective endothelin receptor antagonist with a quinazoline core linked to aromatic substituents and amine groups.

  • Chemical Formula: C₂₄H₂₂N₄O₆S₂

Chemical formula of Tezosentan
Structure of Tezosentan
Structure of Tezosentan

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.

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