||Ambrisentan is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.
||Macitentan is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension (PAH).
||Ro 46-2005 is a synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor, IC50: 220 nM).
||RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition.
||Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.
||Bosentan is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by b
||Bosentan is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.
||Sitaxsentan (sodium) is a highly selective antagonist of endothelin A receptors.
||BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.