Endothelin Receptors

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  1. ETA-receptor Antagonist

    Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
  2. ETAR/ETBR inhibitor

    Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.
  3. EndothelinA receptor antagonist

    Ambrisentan functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA).
  4. Endothelin antagonist

    Avosentan (SPP301) is a potent and highly selective ETA receptor blocker.
  5. Endothelin receptor antagonist

    Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  6. ETA receptor antagonist

    Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.
  7. ET-A and ET-B antagonist

    Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

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