Endothelin receptor antagonist
Template:Short description Template:Cs1 config An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors.
Three main kinds of ERAs exist:
- Dual ET Receptor Antagonists, which affect both endothelin A (ETA) and B receptors (ETB) [2] CPU0213 [821780-32-9] is an example of a dual receptor endothelin receptor antagonist.[3]
- aprocitentan, bosentan, macitentan, tezosentan, Feloprentan (LU-302872 the HCl salt is called LU-420627) [204267-33-4],[4][5]
- Selective ETA Receptor Antagonists, which affect endothelin A receptors
- Selective ETB Receptor Antagonists, which affect endothelin B receptors
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,[8] BMS-193884,[9] BQ-485 [141594-26-5][10] CI 1020 (PD 156707) [162256-50-0][11][12] Enrasentan [167256-08-8],[13] J 104132 [198279-45-7],[14] L-754142 [173450-67-4],[15] PABSA [188710-94-3],[16] PD-155080,[17] SB 209670 [157659-79-5],[18] ZD1611 [186497-38-1][19]
References
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- ↑ 刘立刚, 李瑞文, 吉民 & 华维一, CN1445218 (2003).
- ↑ Endothelin receptor antagonists
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- ↑ Wilhelm Amberg, et al. WO1998009953 (Abbott GmbH and Co KG).
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- ↑ Amy Mae Bunker, et al. U.S. patent 6545150 (2003 to Warner Lambert Co LLC).
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