scholarly journals Endothelin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

2019 ◽  
Vol 2019 (4) ◽  
Author(s):  
Pedro D'Orléans-Juste ◽  
Anthony P. Davenport ◽  
Théophile Godfraind ◽  
Janet J. Maguire ◽  
Eliot H. Ohlstein ◽  
...  
Keyword(s):  
Amino Acid ◽  
Endothelin Receptors ◽  
Endothelin 1 ◽  
Endothelin 3

Endothelin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Endothelin Receptors [24]) are activated by the endogenous 21 amino-acid peptides endothelins 1-3 (endothelin-1, endothelin-2 and endothelin-3).

Renal Expression of mRNAs for Endothelin-1, Endothelin-3 and Endothelin Receptors in NZB/W F1 Mice

1993 ◽  
Vol 16 (5) ◽  
pp. 233-243 ◽  
Author(s):  
Tsukasa Nakamura ◽  
Isao Ebihara ◽  
Mitsumine Fukui ◽  
Shiori Osada ◽  
Yasuhiko Tomino ◽  
...  
Keyword(s):  
Endothelin Receptors ◽  
Endothelin 1 ◽  
Endothelin 3 ◽  
Renal Expression

Immunohistochemical localization of endothelin-1, endothelin-3 and endothelin receptors in human pheochromocytoma and paraganglioma

1997 ◽  
Vol 47 (8) ◽  
pp. 540-546 ◽  
Author(s):  
Kazuo Watanabe ◽  
Hiroyukl Hiraki ◽  
Hiroshi Hasegawa ◽  
Toshitaka Tanigawa ◽  
Iwao Ernura ◽  
...  
Keyword(s):  
Immunohistochemical Localization ◽  
Endothelin Receptors ◽  
Endothelin 1 ◽  
Endothelin 3

Endothelin receptors are modulated in association with endogenous fluctuations in estrogen

1996 ◽  
Vol 271 (5) ◽  
pp. H1999-H2006 ◽  
Author(s):  
D. A. Barber ◽  
G. C. Sieck ◽  
L. A. Fitzpatrick ◽  
V. M. Miller
Keyword(s):  
Smooth Muscle ◽  
Coronary Arteries ◽  
Endothelin Receptors ◽  
Functional Responses ◽  
Endogenous Fluctuations ◽  
Endothelin 1 ◽  
Site Model ◽  
High Affinity ◽  
Endogenous Estrogen ◽  
Endothelin 3

Experiments were designed to determine whether endogenous physiological fluctuations in sex steroid hormones affect expression or functional responses of endothelin receptors. Coronary arteries from sexually mature male, female, and ovariectomized pigs were prepared either for receptor binding or measurement of isometric force in organ chambers. Competitive binding of 125I-labeled endothelin-1 was significant for a one-site model with unlabeled endothelin-1 and a two-site model with unlabeled endothelin-3 and sarafotoxin S6c in all pigs. The total number of binding sites for all endothelin ligands was not different between male and female pigs. Binding affinities for the high-affinity binding site for both endothelin-3 and sarafotoxin S6c were significantly greater (lower inhibition constant) in membranes prepared from female pigs with high endogenous estrogen. In organ chamber experiments, contractions to endothelin-1 but not endothelin-3 or sarafotoxin S6c were significantly greater in coronary arterial rings from female compared with male pigs and were not affected significantly by removal of the endothelium or by treatment of the rings with either indomethacin (10(-5) mol/l) or the combination of indomethacin and NG-monomethyl-L-arginine (10(-4) mol/l). These results suggest endogenous fluctuations in estrogen are associated with an increase in affinity of a high-affinity endothelin receptor in coronary arterial smooth muscle of female pigs. In addition, independent of endogenous estrogen status, coronary arteries from female pigs generate significantly greater contractions to endothelin-1 compared with male pigs. This phenomenon occurs at the level of smooth muscle and is not dependent on the endothelium or synthesis of nitric oxide or prostaglandins.

Characterization of endothelin receptors mediating contraction and relaxation in rabbit saphenous artery and vein

1993 ◽  
Vol 71 (10-11) ◽  
pp. 818-823 ◽  
Author(s):  
Michel Auguet ◽  
Sylvie Delaflotte ◽  
Pierre-Etienne Chabrier ◽  
Pierre Braquet
Keyword(s):  
Smooth Muscle ◽  
Saphenous Vein ◽  
Rank Order ◽  
Endothelin Receptors ◽  
Response Curves ◽  
Endothelin 1 ◽  
The Right ◽  
Endothelin 3 ◽  
Endothelium Dependent Relaxation ◽  
Saphenous Artery

The endothelin receptors in rabbit isolated rings of saphenous artery and saphenous vein have been characterized using endothelin-1, endothelin-2, endothelin-3, sarafotoxin S6c, and BQ123. Although artery rings were more sensitive than those from vein to the contractile action of phenylephrine, endothelin-1 was about three times more potent as a contractile agonist on vein than on artery. In rings precontracted with phenylephrine, carbachol was 10 times more potent in vein than in artery rings to induce endothelium-dependent relaxation. However, in rings precontracted to a similar tone by endothelin-1, the relaxation elicited by carbachol was reduced in the vein but remained unchanged in the artery. In endothelium-denuded saphenous artery, endothelin-1 and endothelin-2 elicited contraction with equal potency, whereas endothelin-3 and sarafotoxin S6c were weak agonists. In saphenous vein, the rank order of sensitivity was sarafotoxin S6c > endothelin-2 > endothelin-1 = endothelin-3, whereas sarafotoxin S6c and, to a lesser extent, endothelin-3 act as partial agonists. The ETA receptor antagonist BQ123 shifted, to the right, the concentration–response curves of endothelin-1 on endothelium-denuded saphenous artery (pA2 = 7.25). In the endothelium-denuded saphenous vein, 10 μM BQ123 shifted to the right only the response to high concentrations of endothelin-1. In vein but not in artery, endothelin-1 and sarafotoxin S6c induced an endothelium-dependent relaxation, which was increased, in the case of endothelin-1, in the presence of BQ123. These results indicate that the rabbit saphenous vein contains a mixed population of ETA and ETB vasoconstrictor receptors located in the smooth muscle cells and vasorelaxant ETB receptors situated on endothelial cells. In contrast, the saphenous artery only possesses smooth muscle cell ETA receptors responsible for constriction.Key words: endothelium, endothelin, vein, artery, BQ123.

Endothelin-1 and endothelin-3 in cirrhosis: Relations to systemic and splanchnic haemodynamics

1995 ◽  
Vol 23 (2) ◽  
pp. 135-144 ◽  
Author(s):  
Søren Møller ◽  
Veit Gülberg ◽  
Jens H. Henriksen ◽  
Alexander L. Gerbes
Keyword(s):  
Endothelin 1 ◽  
Endothelin 3

Endothelin-1, endothelin-3 and their receptors (endothelin A and endothelin B ) in chronic renal transplant rejection in rats 1

2000 ◽  
Vol 13 (3) ◽  
pp. 175-182 ◽  
Author(s):  
Diana Xi Deng ◽  
Jifu Jiang ◽  
Bertha Garcia ◽  
Robert Zhong ◽  
S. Chakrabarti
Keyword(s):  
Renal Transplant ◽  
Transplant Rejection ◽  
Endothelin 1 ◽  
Endothelin A ◽  
Endothelin B ◽  
Endothelin 3 ◽  
Renal Transplant Rejection
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