R&D Systems Inc. Tocris Bioscience Boston Biochem

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

Related Categories

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

Quick Order

Find multiple products by catalog number

divider line

Peptide Hormone Receptors Product Listing

Peptide Hormone Receptor Product Listing

Highlights over 200 products for peptide hormone receptors. Request copy or view PDF today.

divider line

Gut Hormones and the Regulation of Appetite

Written by V.J. Taylor et al

Gut Hormones Poster

'Gut Hormones and the Regulation of Appetite' summarizes the neuropeptide modulators and gut hormones that influence appetite

divider line

7-TM Receptor Signaling

Written by T. Kenakin et al

7-TM Poster

'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy

divider line

VEGF Pathway & Anti-Angiogenic Therapy

Written by N. Ferrara & Y. Crawford

Angiogenesis Poster

A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance.

divider line

New Product Guide

NPG

Highlights over 130 new products added in the second half of 2013. Request a copy or view PDF today.

divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.