Bosentan: A Dual Endothelin Receptor Antagonist with Affinity for Both ETA and ETB Receptors
Endothelin-1 (ET-1) is a peptide that constricts pulmonary blood vessels and raise blood pressure. Two ET-1 receptor subtypes, ET
A and ET
B, mediate the effects of ET-1 in the vascular smooth muscle and endothelium. The actions of ET
A would be vasoconstriction and cell proliferation, while the actions of ET
B would be vasodilatation, antiproliferation, and ET-1 clearance. Bosentan is a dual endothelin receptor antagonist (ERA) with affinity for both endothelin A and B (ET
A and ET
B) receptors. At one time, the anti-fibrotic potential of bosentan was interested. For your reference, ambrisentan [
A2966] is a selective ET
A receptor antagonist. (The product is for research purpose only.)