Mechanism action of Bosentan
Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by binding to ETA and ETB
receptors in the endothelium and vascular smooth muscle. ET-1
concentrations are elevated in plasma and lung tissue of patients with
pulmonary arterial hypertension, suggesting a pathogenic role for ET-1
in this disease. Bosentan is a specific and competitive antagonist at
endothelin receptor types ETA and ETB. Bosentan has a slightly higher affinity for ETA receptors than for ETB receptors.
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