Endothelin Receptors

The endothelin family consists of highly potent vasoconstrictive peptides. Three endogenous isoforms are known to exist - ET-1, ET-2 and ET-3. Due to their physiological role as vasoactive peptides, endothelins have been linked to certain cardiac, vascular and renal diseases; endothelin antagonists may therefore play an important role in the treatment of these conditions. Two distinct endothelin receptors have so far been cloned in mammals, classified as ETA and ETB receptors.

Endothelin Receptor Target Files

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Endothelin receptors are widely expressed in all tissues. They are also localized to non-vascular structures including epithelial cells, glia and neurons. The principal physiological role of endothelin receptors is the maintenance of vascular tone. They also have comitogenic activity, potentiating the effects of other growth factors such as PDGF.

Receptor Subtype ETA Receptors ETB Receptors
Transduction Mechanism 7-TM, ↑ PI turnover → ↑ Ca2+i.c., ↑ Ca2+ influx 7-TM, ↑ PI turnover → ↑ Ca2+i.c., ↑ Ca2+ influx
Primary Locations Vascular smooth muscle Vascular endothelial cells
Tissue Functions Vasoconstriction, positive ionotrope, cell proliferation Vasodilatation, bronchoconstriction, vasoconstriction, cell proliferation
Endogenous Ligand Potency ET-1 = ET-2 > ET-3 ET-1 = ET-2 = ET-3

Key Compounds Ki Values (nM)
Selective ETB Agonists IRL-1620 (1196)
Sarafotoxin S6c (1175)
BQ-3020 (1189)
[Ala1,3,11,15]-Endothelin (1197)
1190
2800
970
2200*
0.016
0.29
0.18
0.33*
ETA Antagonists BQ-123 (1188)
FR 139317 (1210)
BMS 182874 (1441)
Sulfisoxazole (0731)
CI 1020 (2942)
1.4
1
48
600*
0.3*
1500
7300
> 50000
2200*
480*

* IC50 values

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