Ambrisentan (formerly BSF-208075; LU-208075; BSF208075; LU208075; Letairis; Volibris; pulmonext) is a selective antagonist of the endothelin-1 type A receptor (ETA).

Atrasentan HCl, the hydrochloride salt of Atrasentan (NSC-720763; ABT-627; A-147627; trade name: Xinlay), is a novel and selective endothelin receptor antagonist (IC50 = 0.0551 nM for ETA) with anticancer activity.

Bosentan (formerly Ro 47-0203; brand name Tracleer) is a potent, competitive and dual antagonist of endothelin (ET) receptor with anti-hypertensive activity.

RO462005 is an endothelin receptor selective agonist.

BQ-123 (Cyclo(D-trp-D-asp-pro-D-val-leu); BQ123; BQ 123) is a potent and selective antagonist of endothelin A receptor (ETAR) with an IC50 of 7.3 nM.

Zibotentan (formerly known as ZD-4054; ZD4054) is a specific and orally bioavailable Endothelin (ET)A antagonist with potential antitumor activity.

Macitentan n-butyl analogue, an n-butyl derivative of Macitentan, is an ETA/ETB endothelin (ET) receptor dual antagonist that has potential usefulness in the treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

Macitentan (formerly ACT-064992; ACT064992; ACT 064992; Opsumit) is an orally bioavailable and non-peptide, dual antagonist of ETA/ETB endothelin (ET) receptor.

Sitaxentan sodium (formerly IPI-1040; TBC-11251; IPI 1040; TBC11251; Thelin), the sodium salt of Sitaxentan, is a selective and orally bioavailable endothelin A receptor (ETA) antagonist with anti-hypertensive activity.

Endothelin 1 (swine, human), a synthetic 21 amino acid peptide with the sequence of human and swine Endothelin 1 with potent vasoconstrictive action, is a potent endogenous vasoconstrictor.