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Endothelin Receptor Data
| 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
References
Davenport (2000) International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. Pharmacol.Rev. 54 219. Takai et al (1992) A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor. Biochem.Biophys.Res.Comm. 184 953. Williams et al (1993) Characterization of cloned human endothelin receptors. Life Sci. 53 407. Ihara et al (1995) [3H]-BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur.J.Pharmacol. 274 1. Reynolds et al (1995) Pharmacological differences between rat and human endothelin B receptors. Biochem.Biophys.Res.Comm. 209 506. Nakamichi et al (1992) Different distribution of endothelin receptor subtypes in pulmonary tissues revealed by the novel selective ligands BQ-123 and [Ala1,3,11,15]ET-1. Biochem.Biophys.Res.Comm. 182 144. Makatani et al (2000) Effect of a novel bifunctional endothelin receptor antagonist, IRL 3630A, on guinea pig respiratory mechanics. Eur.J.Pharmacol. 406 139. Aramori et al (1993) Subtype selectivity of a novel endothelin antagonist, FR 139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol.Pharmacol. 43 127. Webb et al (1995) BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. J.Pharmacol.Exp.Ther. 272 1124. Chan et al (1994) Identification of a new class of ETA selective endothelin antagonists by pharmacophore screening. Biochem.Biophys.Res.Comm. 201 228.