Target Information

Target General Infomation
Target ID
T23499
Former ID
TTDS00198
Target Name
Endothelin-1 receptor
Gene Name
EDNRA
Synonyms
ET-A; ETA receptor; ETA-R; Endothelin A receptor; Endothelin receptor A; HET-AR; EDNRA
Target Type
Successful
Disease Arrhythmia [ICD9: 427; ICD10: I47-I49]
Cardiovascular disorder [ICD10: I00-I99]
Cerebrovascular disorders [ICD10: I60-I69]
Diabetic nephropathy [ICD9: 250.4; ICD10: E11.21]
Hypertension [ICD9: 401; ICD10: I10-I16]
Hormone resistant prostate cancer [ICD9: 185; ICD10: C61]
Hormone refractory prostate cancer [ICD9: 140-229, 185; ICD10: C61]
Hypotension [ICD9: 458, 796.3; ICD10: I95]
Heart disease [ICD9: 390-429; ICD10: I00-I52]
Myocardial infarction [ICD9: 410; ICD10: I21, I22]
Nerve injury [ICD10: T14.4]
Pulmonary arterial hypertension [ICD9: 416; ICD10: I27.0, I27.2]
Pulmonary hypertension [ICD9: 416; ICD10: I27.0, I27.2]
Prostate cancer [ICD9: 185; ICD10: C61]
Premature labour [ICD9: 644, 765; ICD10: O60.1, P07.3]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Vasospasm following subarachnoid hemorrhage [ICD9: 430, 728.85, 852.0, 852.1; ICD10: I60, P10.3, R25.2, S06.6]
Unspecified [ICD code not available]
Function
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3.
BioChemical Class
GPCR rhodopsin
Target Validation
T23499
UniProt ID
P25101
Sequence
METLCLRASFWLALVGCVISDNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLP
SNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA
SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS
VDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCM
LNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ
RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATM
NSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRS
SHKDSMN
Drugs and Mode of Action
Drug(s) Ambrisentan Drug Info Approved Pulmonary arterial hypertension [536294], [540573]
Bosentan Drug Info Approved Pulmonary arterial hypertension [537041], [540432]
LU302146 Drug Info Approved Pulmonary hypertension [529282], [530258]
Macitentan Drug Info Approved Cardiovascular disorder [532651], [542373], [551871]
Darusentan Drug Info Phase 3 Hypotension [521903], [540446]
PF-1228305 Drug Info Phase 3 Pulmonary hypertension [549974]
BQ-123 Drug Info Phase 2 Pulmonary arterial hypertension [522196], [543354]
FR139317 Drug Info Phase 2 Hypertension [543355], [549735]
PD-145065 Drug Info Phase 2 Hypertension [533860]
PS433540 Drug Info Phase 2 Hypertension [522259]
sparsentan Drug Info Phase 2 Myocardial infarction [527366]
TBC-3711 Drug Info Phase 2 Hypotension [521781]
YM-598 Drug Info Phase 2 Prostate cancer [521539]
ET-1 Drug Info Phase 0 Discovery agent [524736], [543350]
Atrasentan Drug Info Withdrawn from market Hormone refractory prostate cancer [536957], [540426]
Sitaxsentan Drug Info Withdrawn from market Pulmonary arterial hypertension [536294], [540572]
TBC 11251 (TBC) Drug Info Withdrawn from market Pulmonary arterial hypertension [546296], [551871]
Clazosentan Drug Info Discontinued in Phase 3 Vasospasm following subarachnoid hemorrhage [547565]
Zibotentan Drug Info Discontinued in Phase 3 Hormone resistant prostate cancer [540471], [546670]
97-139 Drug Info Discontinued in Phase 2 Cerebrovascular disorders [546634]
Avosentan Drug Info Discontinued in Phase 2 Diabetic nephropathy [543017], [547349]
BMS-193884 Drug Info Discontinued in Phase 2 Pulmonary arterial hypertension [546390]
EDONENTAN HYDRATE Drug Info Discontinued in Phase 2 Pulmonary arterial hypertension [547387]
ENRASENTAN Drug Info Discontinued in Phase 2 Pulmonary arterial hypertension [545770]
J-104132 Drug Info Discontinued in Phase 2 Pulmonary arterial hypertension [546841]
SB-209670 Drug Info Discontinued in Phase 2 Arrhythmia [540461], [545631]
A-216546 Drug Info Discontinued in Phase 1 Solid tumours [546860]
SB-234551 Drug Info Discontinued in Phase 1 Nerve injury [538610], [546574]
ZD-1611 Drug Info Discontinued in Phase 1 Hypotension [546553]
50-235 Drug Info Terminated Hypertension [545617]
BMS-182874 Drug Info Terminated Hypertension [545806]
BQ-518 Drug Info Terminated Hypertension [546191]
BQ610 Drug Info Terminated Discovery agent [545712]
MX-6120 Drug Info Terminated Heart disease [547652]
PD-155080 Drug Info Terminated Hypertension [545967]
PD142893 Drug Info Terminated Discovery agent [545245]
PD156707 Drug Info Terminated Discovery agent [543356], [545965]
Inhibitor 2-HYDROXY-3,5-DIIODOBENZOIC ACID Drug Info [551377]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
Ac-bhg-F-N-Y-Y-W Drug Info [551298]
Ac-w-F-F-N-Y-Y-W Drug Info [551298]
Asterric acid Drug Info [526255]
Bhg-F-N-Y-Y-W Drug Info [551298]
BMS-182874 Drug Info [525859]
Endothelin-2 Drug Info [530519]
ET-1 Drug Info [530519]
PD-163140 Drug Info [551335]
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys) Drug Info [551271]
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Val-Tyr-Phe-Cys) Drug Info [551271]
W-F-F-N--Y-Y-W Drug Info [551298]
Modulator 50-235 Drug Info [533968]
BMS-187308 Drug Info
BMS-193884 Drug Info
Bosentan Drug Info [556264]
BQ-518 Drug Info [533587]
ENRASENTAN Drug Info [526546]
J-104132 Drug Info [525496]
Macitentan Drug Info [532651]
PD-145065 Drug Info [533860]
PD-155080 Drug Info
PS433540 Drug Info
SB-209670 Drug Info [534175]
Antagonist 97-139 Drug Info [526406], [551871]
A-216546 Drug Info [525441], [551871]
Ambrisentan Drug Info [550963]
Atrasentan Drug Info [535545]
Avosentan Drug Info [536328], [536836]
BQ-123 Drug Info [535609], [538019]
BQ610 Drug Info [535521]
Clazosentan Drug Info [528988]
Darusentan Drug Info [528154]
EDONENTAN HYDRATE Drug Info [550931], [551871]
FR139317 Drug Info [535520]
HJP-272 Drug Info [543573]
LU302146 Drug Info [535544]
LU302872 Drug Info [535544]
MX-6120 Drug Info [527075]
PD142893 Drug Info [535521]
PD156707 Drug Info [538130]
PD164333 Drug Info [534570]
PF-1228305 Drug Info [549974]
SB-234551 Drug Info [526119], [551871]
Sitaxsentan Drug Info [536294]
sparsentan Drug Info [527799]
TBC 11251 (TBC) Drug Info [538147]
TBC-3711 Drug Info [526125]
YM-598 Drug Info [544172]
ZD-1611 Drug Info [525566]
Zibotentan Drug Info [550288]
[125I]PD151242 Drug Info [533849]
[125I]PD164333 Drug Info [534570]
[3H]BQ123 Drug Info [533729]
[3H]S0139 Drug Info [543573]
Agonist sarafotoxin S6b Drug Info [533673]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Vascular smooth muscle contraction
Renin secretion
Pathways in cancer
NetPath Pathway IL4 Signaling Pathway
PANTHER Pathway Endothelin signaling pathway
Pathway Interaction Database Endothelins
EGFR-dependent Endothelin signaling events
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways Prostaglandin Synthesis and Regulation
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 521539ClinicalTrials.gov (NCT00050297) YM598 in Patients With Rising PSA After Initial Therapy for Localized Prostate Cancer. U.S. National Institutes of Health.
Ref 521781ClinicalTrials.gov (NCT00272961) A Study Of Different Doses Of TBC3711 In Patients With Uncontrolled High Blood Pressure Already Taking Medications For High Blood Pressure.. U.S. National Institutes of Health.
Ref 521903ClinicalTrials.gov (NCT00389779) DORADO-AC - Optimized Doses of Darusentan as Compared to an Active Control in Resistant Hypertension. U.S. National Institutes of Health.
Ref 522196ClinicalTrials.gov (NCT00586820) Role of Endothelin in Microvascular Dysfunction Following PCI for NSTEMI. U.S. National Institutes of Health.
Ref 522259ClinicalTrials.gov (NCT00635232) A Study To Evaluate The Dose-Related Efficacy and Safety of PS433540 in Subjects With Hypertension. U.S. National Institutes of Health.
Ref 524736ClinicalTrials.gov (NCT02124824) Contribution of Endothelin-1 to Exercise Intolerance in Heart Failure. U.S. National Institutes of Health.
Ref 527366Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.
Ref 5292822007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
Ref 530258Ambrisentan, an endothelin receptor type A-selective endothelin receptor antagonist, for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2009 Aug;10(11):1847-58.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 533860Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065. Br J Pharmacol. 1994 May;112(1):207-13.
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 536957Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27.
Ref 537041Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension. Vasc Health Risk Manag. 2008;4(5):943-52.
Ref 538610(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1000).
Ref 540426(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3487).
Ref 540432(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3494).
Ref 540446(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3508).
Ref 540461(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3528).
Ref 540471(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3539).
Ref 540572(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3950).
Ref 540573(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3951).
Ref 542373(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7352).
Ref 543017(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8260).
Ref 543350(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 989).
Ref 543354(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 997).
Ref 543355(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 998).
Ref 543356(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 999).
Ref 545245Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002573)
Ref 545617Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003913)
Ref 545631Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003996)
Ref 545712Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004314)
Ref 545770Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004637)
Ref 545806Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004811)
Ref 545965Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005545)
Ref 545967Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005553)
Ref 546191Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006825)
Ref 546296Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007312)
Ref 546390Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007870)
Ref 546553Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008908)
Ref 546574Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009010)
Ref 546634Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009311)
Ref 546670Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009560)
Ref 546841Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010566)
Ref 546860Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010699)
Ref 547349Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015393)
Ref 547387Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015788)
Ref 547565Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017374)
Ref 547652Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018158)
Ref 549735Acute Endothelin-Receptor Inhibition Does Not Attenuate Acetylcholine-Induced Coronary Vasoconstriction in Experimental Hypercholesterolemia. Arteriosclerosis, Thrombosis, and Vascular Biology, 1998.18: 108-113.
Ref 549974Pfizer. Product Development Pipeline. March 31 2009.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525441Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201.
Ref 525496Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist. J Pharmacol Exp Ther. 1999 Jun;289(3):1262-70.
Ref 525566Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91.
Ref 525859J Med Chem. 2000 Aug 10;43(16):3111-7.Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.
Ref 526119Effects of the novel selective endothelin ET(A) receptor antagonist, SB 234551, on the cardiovascular responses to endotoxaemia in conscious rats. Br J Pharmacol. 2001 Aug;133(8):1371-7.
Ref 526125TBC3711, an ET(A) receptor antagonist, reduces neonatal hypoxia-induced pulmonary hypertension in piglets. Pediatr Res. 2001 Sep;50(3):374-83.
Ref 526255J Nat Prod. 2002 Jan;65(1):7-10.New chlorinated diphenyl ethers from an Aspergillus species.
Ref 526406S-0139 (Shionogi). Curr Opin Investig Drugs. 2002 Jul;3(7):1051-6.
Ref 526546Enrasentan, an antagonist of endothelin receptors. Cardiovasc Drug Rev. 2003 Spring;21(1):1-16.
Ref 527075Endothelin receptor antagonists in heart failure: current status and future directions. Drugs. 2004;64(10):1029-40.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 528154Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
Ref 528988Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subarachnoid hemorrhage - preliminary results from a randomized clinical series. Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918. Epub 2007 Aug 13.
Ref 530519J Nat Prod. 2009 Dec;72(12):2172-6.5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 533587Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. J Med Chem. 1995 Oct 13;38(21):4309-24.
Ref 533673ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br J Pharmacol. 1995 May;115(1):191-7.
Ref 533729[3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur J Pharmacol. 1995 Feb 14;274(1-3):1-6.
Ref 533849[125I]-PD151242: a selective radioligand for human ETA receptors. Br J Pharmacol. 1994 Jan;111(1):4-6.
Ref 533860Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065. Br J Pharmacol. 1994 May;112(1):207-13.
Ref 533968Structure-activity relationships of an endothelin ETA receptor antagonist, 50-235, and its derivatives. Eur J Pharmacol. 1993 Oct 15;247(2):219-21.
Ref 534175Effects of the endothelin receptor antagonist, SB 209670, on circulatory failure and organ injury in endotoxic shock in the anaesthetized rat. Br J Pharmacol. 1996 May;118(1):198-204.
Ref 534570Characterization of [125I]-PD164333, an ETA selective non-peptide radiolabelled antagonist, in normal and diseased human tissues. Br J Pharmacol. 1998 Jan;123(2):223-30.
Ref 535520Reduction of bFGF-induced smooth muscle cell proliferation and endothelin receptor mRNA expression by mevastatin and atorvastatin. Biochem Pharmacol. 2002 Aug 1;64(3):497-505.
Ref 535521Human optic nerve head astrocytes as a target for endothelin-1. Invest Ophthalmol Vis Sci. 2002 Aug;43(8):2704-13.
Ref 535544Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S.
Ref 535545Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S.
Ref 535609The therapeutic potential of endothelin-1 receptor antagonists and endothelin-converting enzyme inhibitors on the cardiovascular system. Expert Opin Investig Drugs. 2002 Nov;11(11):1537-52.
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 536328Influence of avosentan (SPP3OI) on the pharmacokinetics of a second generation oral contraceptive containing ethinylestradiol and levonorgestrel in healthy female volunteers. Int J Clin Pharmacol Ther. 2006 Dec;44(12):668-74.
Ref 536836Agents in development for the treatment of diabetic nephropathy. Expert Opin Emerg Drugs. 2008 Sep;13(3):447-63.
Ref 538019Endothelin in heart failure: a promising therapeutic target? Heart. 1997 Feb;77(2):93-4.
Ref 538130Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112.
Ref 538147Systemic administration of the endothelin-A receptor antagonist TBC 11251 attenuates cerebral vasospasm after experimental subarachnoid hemorrhage: dose study and review of endothelin-based therapiesin the literature on cerebral vasospasm. Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8.
Ref 543573(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 219).
Ref 544172Role of the endothelin axis and its antagonists in the treatment of cancer. Br J Pharmacol. 2011 May; 163(2): 220-233.
Ref 549974Pfizer. Product Development Pipeline. March 31 2009.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 550931US patent application no. 9,062,094, Dipeptide-based prodrug linkers for aliphatic amine-containing drugs.
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551271Structure-activity relationships in a series of monocyclic endothelin analogues, Bioorg. Med. Chem. Lett. 4(4):567-572 (1994).
Ref 551298Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors, Bioorg. Med. Chem. Lett. 5(6):621-626 (1995).
Ref 551335gamma-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs, Bioorg. Med. Chem. Lett. 7(3):297-302 (1997).
Ref 551377Allosteric inhibition of endothelin <span class="caps">ETA</span> receptors by 3, 5-dibromosalicylic acid. Mol Pharmacol. 2000 Dec;58(6):1461-9.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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