An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors.
Classes
Three main kinds of ERAs exist:
Dual ET Receptor Antagonists, which affect both endothelin A (ETA) and B receptors (ETB)Endothelin receptor antagonists CPU0213 [821780-32-9] is an example of a dual receptor endothelin receptor antagonist. aprocitentan, bosentan, macitentan, tezosentan, Feloprentan (LU-302872 the HCl salt is called LU-420627) [204267-33-4],Wilhelm Amberg, et al. WO1998009953 (Abbott GmbH and Co KG). Selective ETA Receptor Antagonists, which affect endothelin A receptors sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan, clazosentan, fandosentan,Amy Mae Bunker, et al. (2003 to Warner Lambert Co LLC). diosuxentan. Selective ETB Receptor Antagonists, which affect endothelin B receptors BQ-788 and A192621 are used in research but have not yet reached clinical trial stage
Macitentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension, while atrasentan is an experimental anti-cancer drug.
Further (unsorted) examples include: BMS-182874, BMS-193884, BQ-485 [141594-26-5] CI 1020 (PD 156707) [162256-50-0] Enrasentan [167256-08-8], J 104132 [198279-45-7], L-754142 [173450-67-4], PABSA [188710-94-3], PD-155080, SB 209670 [157659-79-5], ZD1611 [186497-38-1]
References