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Endothelins in the Lung
Published in Sami I. Said, Proinflammatory and Antiinflammatory Peptides, 2020
Peter J. Henry, Roy G. Goldie, Douglas W. P. Hay
Stx S6b and Stx S6c have significant sequence homology with the ETs (75). As with ET-1, Stx S6b is an agonist which does not discriminate between ETA and ETB receptor subtypes, whereas Stx S6c is highly selective for the ETB receptor subtype (76). The synthetic linear peptides BQ-3020 (77) and IRL-1620 (78) are also selective ETB receptor agonists (Table 1). Of the available ETA receptor-selective antagonists, the cyclic pentapeptide BQ-123 (79) is the most commonly used and the best characterized. Several peptide ETB receptor-selective antagonists have also been developed, with the tripeptide BQ-788 being the current “gold standard” in this group (80). Other ETB receptor-selective antagonists include the 16-amino acid peptide RES-701–1, purified from the culture broth of Streptomyces sp. (81,82).
Endothelin and Cardiac Hypertrophy
Published in Malcolm J. Lewis, Ajay M. Shah, Endothelial Modulation of Cardiac Function, 2020
Recent extensive studies have developed a variety of receptor antagonists and agonists specific for each ET receptor subtype, such as the ETA antagonist BQ123 (Ihara et al., 1992), the ETB agonist BQ3020 (Ihara et al., 1992), and the ETB antagonist BQ788 (Ishikawa et al., 1994). These receptor subtype-specific antagonists and agonists have opened a new avenue for pharmacological and molecular biological studies with ETs.
The effect of endothelin receptor antagonists in the endotoxin-induced uveitis rabbit model*
Published in Cutaneous and Ocular Toxicology, 2018
Emine Esra Karaca, Feyzahan Uzun, Ergin Dileköz, Gökçe Sevim Öztürk Fincan, Sevim Ercan, Oğuz Kul, Emin Ümit Bağrıaçık, Meral Or
Endothelin-1, found in several ocular tissues, also expressed by cardiac tissue, macrophages, leukocytes, fibroblasts and astrocytes; is the most known vasoconstrictor substance1,27–29. Studies have shown that ET-1 plays a role in aqueous outflow, chorioretinal circulation, pupil diameter, corneal epithelium and endothelial proliferation, aqueous protein concentration and intraocular inflammation2,11. After the identification of ET-1 receptors, selective and nonselective use of ET receptor antagonists has come to the fore. In a study by Shoji et al.30, 97–139, the ETA receptor antagonist, was observed to decrease the amount of aqueous protein and PGE2 but the ETB receptor antagonist BQ788 did not reduce the inflammatory response.
Effects Of Endothelin-1 On Intracellular Tetrahydrobiopterin Levels In Vascular Tissue
Published in Scandinavian Cardiovascular Journal, 2018
Ruha Cerrato, Mark Crabtree, Charalambos Antoniades, Karolina Kublickiene, Ernesto L. Schiffrin, Keith M. Channon, Felix Böhm
In a separate set of experiments, additional rings were analyzed after 20 min preincubation with either the ETA receptor antagonist BQ123 (1 μM) alone, or in combination with the ETB receptor antagonist BQ788 (1 μM; dual BQ) followed by ET-1 (0.1 nM) infusion for 45 min. At the end of these experiments, the NADPH-stimulated superoxide production was estimated 10 min after NADPH (0.1mM) was added as previously described [13].