Nomenclature: ETA receptor

Family: Endothelin receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 427 4q31.22 EDNRA endothelin receptor type A 1,10,27,56
Mouse 7 427 8 Ednra endothelin receptor type A 41
Rat 7 426 19q11 Ednra endothelin receptor type A 32
Previous and Unofficial Names
ENDOR
ET-A
ET-AR
Eta
RATENDOR
RGD1559432
endothelin A receptor
endothelin-1 receptor
endothelin-1 receptor-like
Gpcr10
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
endothelin-1 {Sp: Human, Mouse, Rat}
endothelin-2 {Sp: Human}
Comments: endothelin-3 is a low potency endogenous agonist
Family selective agonists (Human)
ET-1 (EDN1, P05305) = ET-2 (EDN2, P20800) > ET-3 (EDN3, P14138)  [34]
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]ET-1 Hs Full agonist 9.1 – 10.5 pKd 18,30-31
pKd 9.1 – 10.5 [18,30-31]
[125I]sarafotoxin S6b Hs Full agonist 9.6 – 9.8 pKd 2
pKd 9.6 – 9.8 [2]
[125I]ET-2 Hs Full agonist 8.9 – 9.1 pKd 2
pKd 8.9 – 9.1 [2]
[18F]ET-1 Hs Full agonist 8.2 pKd 29
pKd 8.2 [29]
endothelin-2 {Sp: Human} Hs Full agonist 8.2 pIC50 34
pIC50 8.2 [34]
endothelin-1 {Sp: Human, Mouse, Rat} Hs Full agonist 7.8 – 8.5 pIC50 34
pIC50 7.8 – 8.5 [34]
sarafotoxin S6b Hs Full agonist 7.5 – 8.1 pIC50 34
pIC50 7.5 – 8.1 [34]
Agonist Comments
In mammals, the endothelin (ET) family comprises three endogenous isoforms, ET-1, ET-2 and ET-3. ET-1 is the principal isoform in the human cardiovascular system and is one of the most ubiquitous, potent and unusually long lasting constrictor of human vessels. ET-2 has been less extensively studied than other ET peptides but the peptide is present in human cardiovascular tissues and ET-2 was as potent a vasoconstrictor as ET-1 in human arteries and veins. VIC (vasoactive intestinal contractor) is the murine isoform of ET-2. Endothelial cells do not synthesise ET-3 but the mature peptide is detectable in plasma and other tissues including heart and brain. ET-3 is unique in that it is the only endogenous isoform that distinguishes between the two endothelin receptors. It has the same affinity at the ETB receptor as ET-1 but, at physiological concentrations, has little or no affinity for the ETA.The only endogenous peptides with a high degree of sequence similarity to the ETs are the sarafotoxins (S6a, S6b, S6c, S6d). This family of 21aa peptides were originally discovered in the venom of a snake, Atractaspis engadensis [12].
ETA receptors are initially classfied according to the the rank order of potency of ET agonists with ET-1 being equipotent to ET-2 but ET-3 typically displaying 100 fold less potency and confirmed by using selective peptide antagonists (eg BQ123 and FR139317) or non-peptide antagonists (eg PD156707 or A127722).
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
A127722 Hs Antagonist 9.2 – 10.5 pA2 42
pA2 9.2 – 10.5 [42]
PD-156707 Hs Antagonist 8.1 – 9.2 pA2 35,44
pA2 8.1 – 9.2 [35,44]
TAK 044 Rn Antagonist 8.4 pA2 51
pA2 8.4 [51]
sitaxsentan Hs Antagonist 8.0 pA2 52
pA2 8.0 [52]
bosentan Rn Antagonist 7.2 pA2 8
pA2 7.2 [8]
BQ123 Hs Antagonist 6.9 – 7.4 pA2 34
pA2 6.9 – 7.4 [34]
ambrisentan Hs Antagonist 7.1 pA2 6
pA2 7.1 [6]
SB209670 Rn Antagonist 9.4 pKB 23
pKB 9.4 (KB 4x10-10 M) [23]
[125I]PD164333 Hs Antagonist 9.6 – 9.8 pKd 14
pKd 9.6 – 9.8 (Kd 1.58x10-10 – 2.5x10-10 M) [14]
PD-156707 Hs Antagonist 9.0 – 9.8 pKd 35
pKd 9.0 – 9.8 (Kd 1.5x10-10 – 9.2x10-10 M) [35]
[125I]PD151242 Hs Antagonist 9.0 – 9.1 pKd 15
pKd 9.0 – 9.1 (Kd 7.9x10-10 – 1x10-9 M) [15]
[3H]BQ123 Hs Antagonist 8.5 pKd 28
pKd 8.5 (Kd 3.2x10-9 M) [28]
darusentan Hs Antagonist 8.9 pKi 46
pKi 8.9 [46]
macitentan Hs Antagonist 9.3 pIC50 5
pIC50 9.3 (IC50 5x10-10 M) [5]
SB234551 Hs Antagonist 8.7 – 9.0 pIC50 39
pIC50 8.7 – 9.0 [39]
zibotentan Hs Antagonist 8.3 pIC50 37
pIC50 8.3 [37]
ambrisentan Hs Antagonist 7.66 pIC50 6
pIC50 7.66 (IC50 2.17x10-8 M) [6]
FR139317 Hs Inverse agonist 7.3 – 7.9 pIC50 34
pIC50 7.3 – 7.9 [34]
View species-specific antagonist tables
Antagonist Comments
Antagonists are currently classified as either ETA-selective, ETB-selective or mixed antagonists that display similar affinity for both receptors. The most highly selective peptide antagonists (4-5 orders of selectivity) for the ETA receptors are the cyclic pentapeptide, BQ123 and the modified linear peptide FR139317. Unlike peptide antagonists, many non-peptide ETA receptor-selective antagonists have oral bioavalibility and some may cross the blood brain barrier. [4,11-13,24,53]. The approved drug, macitentan, is a dual endothelin receptor antagonist [5] with higher affinity for the ETA receptor than for the ETB receptor (IC50 0.5nM and 391nM respectively) [5].
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Phospholipase A2 stimulation
Phospholipase D stimulation
Comments:  Activation of ETA receptors to produce a range of biological actions in different tissues is thought to be mediated by a number of transduction systems coupled to various types of G-protein, predominatly Gq/11 but there is also evidence for Gi/o (lactotrophs, myocytes), Gi2 and Gs. The major enzyme systems activated include phospholipase C, A2 and D. Calcium signalling is a nearly universal response for ET-1 induced vasoconstriction via generation of IP3 and DAG whereas cyclic nucleotide levels often remain unaltered. ET-1 also has mitogenic actions leading to cell proliferation [22,45,49-50]
References:  22,45,49-50
Tissue Distribution
ETA receptors are mainly localised to vascular smooth muscle cells (where they are the predominant sub-type) and therefore in all tissues receiving a blood supply including heart, lung and brain. ETA receptors are also present on other cell types including myocytes within the heart.
Species:  Human
Technique:  Radioligand binding
References:  19
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Isolated ring preparations of human coronary artery.
Species:  Human
Tissue:  Coronary artery.
Response measured:  Vasoconstriction.
References:  34
Isolated ring preparations of rat thoracic aorta.
Species:  Rat
Tissue:  Aorta.
Response measured:  Vasoconstriction.
References:  20,38,43
Physiological Functions
Positive inotrope.
Species:  Rat
Tissue:  Heart.
References:  36
Vasoconstrictor.
Species:  Mouse
Tissue:  Blood vessels.
References:  47
Vasoconstrictor.
Species:  Human
Tissue:  Blood vessels.
References:  26,34
Positive inotrope.
Species:  Human
Tissue:  Heart.
References:  21,33,36
Vasoconstrictor.
Species:  Rat
Tissue:  Blood vessels.
References:  20,25,38,43
Cell proliferation/mitogenic effects.
Species:  Human
Tissue:  Smooth muscle cells from a range of vascular beds, fibroblasts, cancer cells.
References:  54
Physiological Consequences of Altering Gene Expression
Mice deficient for ETA receptor, mimic the human conditions collectively termed CATCH 22 or velocardiofacial syndrome, which includes severe craniofacial deformities and defects in the cardiovascular outflow tract. Great vessel malformations highly similar to those seen in neural crest-ablated chick embryos and human congenital cardiac defect also occur.
Species:  Mouse
Tissue: 
Technique:  Not specified
References:  7,55
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0010465 aberrant origin of the right subclavian artery PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0003235 abnormal alisphenoid bone morphology PMID: 15306564 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0003235 abnormal alisphenoid bone morphology PMID: 18199583 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0004189 abnormal alveolar process PMID: 18199583 
Ednratm1Ywa|Ednrbtm1Ywa Ednratm1Ywa/Ednratm1Ywa,Ednrbtm1Ywa/Ednrbtm1Ywa
involves: 129S/SvEv
MGI:102720  MGI:105923  MP:0002191 abnormal artery morphology PMID: 9449665 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0002191 abnormal artery morphology PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0009867 abnormal ascending aorta morphology PMID: 9649553 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0000106 abnormal basisphenoid bone morphology PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0002672 abnormal branchial arch artery morphology PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0002127 abnormal cardiovascular system morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004181 abnormal carotid artery morphology PMID: 9449664 
Ednratm2.1Hku|Ednratm3(Ednrb)Hku Ednratm2.1Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002116 abnormal craniofacial bone morphology PMID: 18199583 
Ednratm3(Ednrb)Hku Ednratm3(Ednrb)Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002116 abnormal craniofacial bone morphology PMID: 18199583 
Ednratm2Hku|Ednratm3(Ednrb)Hku Ednratm2Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002116 abnormal craniofacial bone morphology PMID: 18199583 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0002116 abnormal craniofacial bone morphology PMID: 19185569 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0000428 abnormal craniofacial morphology PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004787 abnormal dorsal aorta morphology PMID: 9449664 
Ednratm1Ywa|Foxc2tm1Miu Ednratm1Ywa/Ednratm1Ywa,Foxc2tm1Miu/Foxc2tm1Miu
involves: C57BL/6
MGI:105923  MGI:1347481  MP:0004787 abnormal dorsal aorta morphology PMID: 15664398 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0001071 abnormal facial nerve morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0006337 abnormal first branchial arch morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0006354 abnormal fourth branchial arch artery morphology PMID: 9649553 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0003056 abnormal hyoid bone morphology PMID: 18199583 
Ednratm2.1Hku|Ednratm3(Ednrb)Hku Ednratm2.1Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0003056 abnormal hyoid bone morphology PMID: 18199583 
Ednratm3(Ednrb)Hku Ednratm3(Ednrb)Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0003056 abnormal hyoid bone morphology PMID: 18199583 
Ednratm2Hku|Ednratm3(Ednrb)Hku Ednratm2Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0003056 abnormal hyoid bone morphology PMID: 18199583 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0005358 abnormal incisor morphology PMID: 19185569 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0005106 abnormal incus morphology PMID: 19185569 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0000029 abnormal malleus morphology PMID: 18199583 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0000029 abnormal malleus morphology PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0000458 abnormal mandible morphology PMID: 15306564 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0000458 abnormal mandible morphology PMID: 18199583 
Ednratm2.1Hku|Ednratm3(Ednrb)Hku Ednratm2.1Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0000458 abnormal mandible morphology PMID: 18199583 
Ednratm3(Ednrb)Hku Ednratm3(Ednrb)Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0000458 abnormal mandible morphology PMID: 18199583 
Ednratm2Hku|Ednratm3(Ednrb)Hku Ednratm2Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0000458 abnormal mandible morphology PMID: 18199583 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0000458 abnormal mandible morphology PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0001068 abnormal mandibular nerve branching PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0000455 abnormal maxilla morphology PMID: 15306564 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0005587 abnormal Meckel's cartilage morphology PMID: 15306564 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0005105 abnormal middle ear ossicle morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0000452 abnormal mouth morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0000452 abnormal mouth morphology PMID: 15306564 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0000452 abnormal mouth morphology PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0002108 abnormal muscle morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0002177 abnormal outer ear morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0003755 abnormal palate morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0005249 abnormal palatine bone morphology PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0005249 abnormal palatine bone morphology PMID: 15306564 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0005249 abnormal palatine bone morphology PMID: 18199583 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0004452 abnormal pterygoid process morphology PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0002327 abnormal respiratory function PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0006355 abnormal sixth branchial arch artery morphology PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0005508 abnormal skeleton morphology PMID: 9449664 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0004423 abnormal squamosal bone morphology PMID: 18199583 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0005107 abnormal stapes morphology PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0008023 abnormal styloid process morphology PMID: 9449664 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0008023 abnormal styloid process morphology PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0006356 abnormal third branchial arch artery morphology PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0001065 abnormal trigeminal nerve morphology PMID: 9449664 
Ednratm2Ywa|Tg(Aqp2-cre)1Dek Ednratm2Ywa/Ednratm2Ywa,Tg(Aqp2-cre)1Dek/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL
MGI:105923  MGI:3712434  MP:0002987 abnormal urine osmolality PMID: 15928212 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0005270 abnormal zygomatic bone morphology PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0008381 absent gonial bone PMID: 15306564 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0008381 absent gonial bone PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004318 absent incus PMID: 9449664 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0004318 absent incus PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004319 absent malleus PMID: 9449664 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0004319 absent malleus PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004439 absent Meckel's cartilage PMID: 9449664 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0004439 absent Meckel's cartilage PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0010486 absent right subclavian artery PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0000614 absent salivary gland PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004204 absent stapes PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0006019 absent tympanic membrane PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0003138 absent tympanic ring PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0003138 absent tympanic ring PMID: 15306564 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0003138 absent tympanic ring PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0010543 aorta tubular hypoplasia PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0000114 cleft chin PMID: 9449664 
Ednratm1Ywa|Foxc2tm1Miu Ednratm1Ywa/Ednratm1Ywa,Foxc2tm1Miu/Foxc2tm1Miu
involves: C57BL/6
MGI:105923  MGI:1347481  MP:0003140 dilated heart atrium PMID: 15664398 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0004159 double aortic arch PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0000284 double outlet heart right ventricle PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0000284 double outlet heart right ventricle PMID: 9649553 
Ednratm1Ywa|Foxc2tm1Miu Ednratm1Ywa/Ednratm1Ywa,Foxc2tm1Miu/Foxc2tm1Miu
involves: C57BL/6
MGI:105923  MGI:1347481  MP:0006207 embryonic lethality during organogenesis PMID: 15664398 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0008797 facial cleft PMID: 19185569 
Ednratm2Ywa|Tg(Aqp2-cre)1Dek Ednratm2Ywa/Ednratm2Ywa,Tg(Aqp2-cre)1Dek/0
involves: 129S7/SvEvBrd * C57BL/6 * SJL
MGI:105923  MGI:3712434  MP:0005610 increased circulating antidiuretic hormone level PMID: 15928212 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0010544 interrupted aorta PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0000460 mandible hypoplasia PMID: 9449664 
Ednratm2Ywa|Tg(Myh6-cre)2182Mds Ednratm2Ywa/Ednratm2Ywa,Tg(Myh6-cre)2182Mds/0
involves: 129S6/SvEvTac * C57BL/6J * FVB/N
MGI:105923  MGI:2447636  MP:0002169 no abnormal phenotype detected PMID: 14585980 
Ednratm2Ywa Ednratm2Ywa/Ednratm2Ywa
involves: 129S6/SvEvTac * C57BL/6J * FVB/N
MGI:105923  MP:0002169 no abnormal phenotype detected PMID: 14637162 
Ednratm2Ywa|Tg(AQP2-cre)2Dek Ednratm2Ywa/Ednratm2Ywa,Tg(AQP2-cre)2Dek/0
involves: 129S6/SvEvTac * C57BL/6 * CBA
MGI:105923  MGI:3054060  MP:0002169 no abnormal phenotype detected PMID: 16868309 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0000273 overriding aorta PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0000273 overriding aorta PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0003139 patent ductus arteriosus PMID: 9449664 
Ednratm1Ywa|Foxc2tm1Miu Ednratm1Ywa/Ednratm1Ywa,Foxc2tm1Miu/Foxc2tm1Miu
involves: C57BL/6
MGI:105923  MGI:1347481  MP:0001787 pericardial edema PMID: 15664398 
Ednratm1Ywa|Ednrbtm1Ywa Ednratm1Ywa/Ednratm1Ywa,Ednrbtm1Ywa/Ednrbtm1Ywa
involves: 129S/SvEv
MGI:102720  MGI:105923  MP:0005312 pericardial effusion PMID: 9449665 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0010418 perimembraneous ventricular septal defect PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0002081 perinatal lethality PMID: 9449664 
Ednratm1Hku Ednratm1Hku/Ednratm1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm2.1Hku Ednratm2.1Hku/Ednratm2.1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm1Hku|Ednratm2.1Hku Ednratm1Hku/Ednratm2.1Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm2.1Hku|Ednratm3(Ednrb)Hku Ednratm2.1Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm3(Ednrb)Hku Ednratm3(Ednrb)Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm1Hku|Ednratm3(Ednrb)Hku Ednratm1Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm2Hku Ednratm2Hku/Ednratm2Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm2Hku|Ednratm3(Ednrb)Hku Ednratm2Hku/Ednratm3(Ednrb)Hku
involves: 129 * C57BL/6 * ICR
MGI:105923  MP:0002081 perinatal lethality PMID: 18199583 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0010572 persistent right dorsal aorta PMID: 9649553 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0002633 persistent truncus arteriosis PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
involves: 129S/SvEv * C57BL/6 * CBA
MGI:105923  MP:0002633 persistent truncus arteriosis PMID: 9649553 
Ednratm1Ywa|Foxc2tm1Miu Ednratm1Ywa/Ednratm1Ywa,Foxc2tm1Miu/Foxc2tm1Miu
involves: C57BL/6
MGI:105923  MGI:1347481  MP:0002633 persistent truncus arteriosis PMID: 15664398 
Ednratm1Ywa|Ednrbtm1Ywa Ednratm1Ywa/Ednratm1Ywa,Ednrbtm1Ywa/Ednrbtm1Ywa
involves: 129S/SvEv
MGI:102720  MGI:105923  MP:0002080 prenatal lethality PMID: 9449665 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0000088 short mandible PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0006344 small second branchial arch PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004468 small zygomatic bone PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
Not Specified
MGI:105923  MP:0004468 small zygomatic bone PMID: 15306564 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0001823 thymus hypoplasia PMID: 9449664 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0009904 tongue hypoplasia PMID: 9449664 
Ednratm2Ywa|Tg(Wnt1-cre)11Rth Ednratm2Ywa/Ednratm2Ywa,Tg(Wnt1-cre)11Rth/0
involves: C57BL/6J * CBA/J
MGI:105923  MGI:2447280  MP:0009904 tongue hypoplasia PMID: 19185569 
Ednratm1Ywa Ednratm1Ywa/Ednratm1Ywa
129S/SvEv
MGI:105923  MP:0004110 transposition of great arteries PMID: 9449664 
Biologically Significant Variants
Type:  Splice variants.
Species:  Human
Description:  A gene encoding a truncated (109 amino acids deleted) ETA receptor was more abundant than the wild type in melanoma cell lines and tissue. The expressed receptor did not bind ET-1, suggesting reduced responsiveness to ET-1 in these tumours.
References:  57
General Comments
Antagonists that block both ETA and ETB receptors (also called mixed or balanced) include peptides such as TAK044. Non-peptide compounds included bosentan (RO470203, Tracleer [8]) the first antagonist in clinical use [16] SB209670 [23], SB217242 (enrasentan, [40]) and RO610612 (tezosentan, [9]). The distinction between antagonists that are ETA selective and those that block both ETAand ETB receptors is not precise but generally the former display greater than 100-fold selectivity for the ETAsubtype and the latter less than 100-fold.

For reviews on endothelin receptors see [3,17,48].
Available Assays
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To cite this database page, please use the following:

Anthony P. Davenport, Pedro D'Orléans-Juste, Théophile Godfraind, Janet J. Maguire, Eliot H. Ohlstein, Robert R. Ruffolo.
Endothelin receptors: ETA receptor. Last modified on 23/05/2014. Accessed on 21/08/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=219.

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