View source for Endothelin receptor antagonist

{{Short description|Drug that blocks endothelin receptors}}
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An '''endothelin receptor antagonist''' ('''ERA''') is a [[medication|drug]] that blocks [[endothelin receptor]]s.

Three main kinds of ERAs exist: 
[[File:CPU0213.svg|thumb|[[CPU0213]]<ref>刘立刚, 李瑞文, 吉民 & 华维一, CN1445218 (2003).</ref> also c.f. [https://pubchem.ncbi.nlm.nih.gov/compound/9892180 CPU 86017] ]]
* Dual ET Receptor Antagonists, which affect both [[Endothelin A receptor|endothelin A]] (ET<sub>A</sub>) and [[Endothelin receptor type B|B receptors]] (ET<sub>B</sub>) <ref>[http://cvpharmacology.com/vasodilator/ETblockers.htm Endothelin receptor antagonists<!-- Bot generated title -->]</ref> [https://pubchem.ncbi.nlm.nih.gov/compound/24864086 CPU0213] [821780-32-9] is an example of a dual receptor endothelin receptor antagonist.<ref name="pmid21915473">{{cite journal | vauthors = Wang ZY, Zhang W, Li XZ, Han Y, Chen YP, Liu Z, Xie LP, Ji Y, Lu X | title = CPU0213, a novel endothelin type A and type B receptor antagonist, protects against myocardial ischemia/reperfusion injury in rats | journal = Brazilian Journal of Medical and Biological Research | volume = 44 | issue = 11 | pages = 1148–55 | date = November 2011 | pmid = 21915473 | doi = 10.1590/s0100-879x2011007500119 | doi-access = free }}</ref>
** [[aprocitentan]], [[bosentan]], [[macitentan]], [[tezosentan]], [[Feloprentan]] (LU-302872 the HCl salt is called LU-420627) [204267-33-4],<ref>{{cite journal | doi=10.1021/jm9910425 | title=Discovery and Synthesis of ( ''S'' )-3-&#91;2-(3,4-Dimethoxyphenyl)ethoxy&#93;-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic Acid (LU 302872), a Novel Orally Active Mixed ET<sub>A</sub>/ET<sub>B</sub> Receptor Antagonist | date=1999 | journal=Journal of Medicinal Chemistry | volume=42 | issue=16 | pages=3026–3032 | pmid=10447946 | vauthors = Amberg W, Hergenröder S, Hillen H, Jansen R, Kettschau G, Kling A, Klinge D, Raschack M, Riechers H, Unger L }}</ref><ref>Wilhelm Amberg, et al. WO1998009953 (Abbott GmbH and Co KG).</ref>
* Selective ET<sub>A</sub> Receptor Antagonists, which affect [[Endothelin receptor type A|endothelin A receptors]]
** [[sitaxentan]], [[ambrisentan]], [[atrasentan]], [[BQ-123]], [[sparsentan]], [[zibotentan]], [[avosentan]], [[edonentan]], [[clazosentan]], [[Fandosentan]]<ref>{{cite journal | vauthors = Jacks TE, Belmont DT, Briggs CA, Horne NM, Kanter GD, Karrick GL, Krikke JJ, McCabe RJ, Mustakis JG, Nanninga TN, Risedorph GS | title = Development of a scalable process for CI-1034, an endothelin antagonist. | journal = Organic Process Research & Development | date = March 2004 | volume = 8 | issue = 2 | pages = 201–212 | doi = 10.1021/op034104g }}</ref><ref>Amy Mae Bunker, et al. {{US patent|6545150}} (2003 to Warner Lambert Co LLC).</ref>
* Selective ET<sub>B</sub> Receptor Antagonists, which affect [[Endothelin receptor type B|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]],<ref>{{cite journal | vauthors = Stein PD, Hunt JT, Floyd DM, Moreland S, Dickinson KE, Mitchell C, Liu EC, Webb ML, Murugesan N, Dickey J | title = The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide | journal = Journal of Medicinal Chemistry | volume = 37 | issue = 3 | pages = 329–331 | date = February 1994 | pmid = 8308857 | doi = 10.1021/jm00029a001 }}</ref> [[BMS-193884]],<ref>{{cite journal | vauthors = Murugesan N, Gu Z, Stein PD, Spergel S, Mathur A, Leith L, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Morrison RA, Webb ML, Moreland S, Barrish JC | title = Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists | journal = Journal of Medicinal Chemistry | volume = 43 | issue = 16 | pages = 3111–3117 | date = August 2000 | pmid = 10956219 | doi = 10.1021/jm000105c }}</ref> [[BQ-485]] [141594-26-5]<ref>{{cite patent | inventor = Clozel JP | number = 5696116 | year = 1997 | country = US | assignee = F Hoffmann La Roche AG }}</ref> [[CI 1020]] (PD 156707) [162256-50-0]<ref>{{cite journal | vauthors = Doherty AM, Patt WC, Edmunds JJ, Berryman KA, Reisdorph BR, Plummer MS, Shahripour A, Lee C, Cheng XM, Walker DM | title = Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists | journal = Journal of Medicinal Chemistry | volume = 38 | issue = 8 | pages = 1259–1263 | date = April 1995 | pmid = 7731010 | doi = 10.1021/jm00008a002 }}</ref><ref>{{cite journal | vauthors = Patt WC, Cheng XM, Repine JT, Lee C, Reisdorph BR, Massa MA, Doherty AM, Welch KM, Bryant JW, Flynn MA, Walker DM, Schroeder RL, Haleen SJ, Keiser JA | title = Butenolide endothelin antagonists with improved aqueous solubility | journal = Journal of Medicinal Chemistry | volume = 42 | issue = 12 | pages = 2162–2168 | date = June 1999 | pmid = 10377221 | doi = 10.1021/jm980504w }}</ref> [[Enrasentan]] [167256-08-8],<ref>{{cite patent | inventor = Andemichael YW | number = 6288247 | year = 2001 | country = US | assignee = SmithKline Beecham Corp }}</ref> [[J 104132]] [198279-45-7],<ref>{{cite patent | inventor = Devine PN | number = 6022972 | year = 2000 | country = US | assignee = Merck and Co Inc }}</ref> [[L-754142]] [173450-67-4],<ref>{{cite patent | inventor = Bagley SW | number = 1994021590 | year = 1994 | country = WO | assignee = Merck and Co Inc }}</ref> [[PABSA]] [188710-94-3],<ref>{{cite journal | vauthors = Iwasaki T, Hayasaki-Kajiwara Y, Matsuo Y, Nakajima M | title = Endothelin receptor antagonist activity of (R)-(-)-2-(benzo[1,3]dioxol-5-yl)-N-(4-isopropylphenylsulfonyl)-2-(6-methyl- 2-propylpyridin-3-yloxy)acetamide hydrochloride (PABSA) in rat aortic smooth muscle cells and isolated rat thoracic aorta | journal = Arzneimittel-Forschung | volume = 51 | issue = 7 | pages = 529–534 | year = 2001 | pmid = 11505783 | doi = 10.1055/s-0031-1300076 }}</ref> [[PD-155080]],<ref>{{cite patent | inventor = Berryman KA | number = 1995005376 | year = 1995 | country = WO | assignee = Warner Lambert Co LLC }}</ref> [[SB 209670]] [157659-79-5],<ref>{{cite patent | inventor = Cousins RD | number = 6448260 | year = 2002 | country = US | assignee = SmithKline Beecham Corp }}</ref> [[ZD1611]] [186497-38-1]<ref>{{cite patent | inventor = Bradbury RH | number = 1996040681 | year = 1996 | country = WO | assignee = AstraZeneca UK Ltd, Syngenta Ltd }}</ref>

==References==
{{Reflist}}

{{PAH rx}}
{{Antihypertensives and diuretics}}

[[Category:Endothelin receptor antagonists| ]]


{{cardiovascular-system-drug-stub}}