ArticleBritish journal of pharmacology1996
Characterization of the endothelin receptor selective agonist, BQ3020 and antagonists BQ123, FR139317, BQ788, 50235, Ro462005 and bosentan in the heart.
Article in British journal of pharmacology, 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed, 48 citations in OpenAlex.
- Kinetics of endothelin-1 and effect selective ETFrontiers in pharmacology · 2024Article
- Endothelin-1 inhibits size dependent lymphatic clearance of PEG-based conjugates after intra-articular injection into the rat knee.Acta biomaterialia · 2019Article
- Evidence for biased agonists and antagonists at the endothelin receptors.Life sciences · 2016Review
- Endothelin.Pharmacological reviews · 2016Review
- Endothelin@25 - new agonists, antagonists, inhibitors and emerging research frontiers: IUPHAR Review 12.British journal of pharmacology · 2014Review
- Modulation of endothelin receptors in the failing right ventricle of the heart and vasculature of the lung in human pulmonary arterial hypertension.Life sciences · 2014Article
- Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy.The American journal of pathology · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Impaired stimulatory effect of ETB receptor on D₃ receptor in immortalized renal proximal tubule cells of spontaneously hypertensive rats.Kidney & blood pressure research · 2011Article
- Inhibitory effect of ETB receptor on Na(+)-K(+) ATPase activity by extracellular Ca(2+) entry and Ca(2+) release from the endoplasmic reticulum in renal proximal tubule cells.Hypertension research : official journal of the Japanese Society of Hypertension · 2009Article
- Renal D3 dopamine receptor stimulation induces natriuresis by endothelin B receptor interactions.Kidney international · 2008Article
- Blood pressure response to type A endothelin receptor antagonism in human obesity and diabetes mellitus.Journal of human hypertension · 2006Article
- Positron emission tomography using 18F-labelled endothelin-1 reveals prevention of binding to cardiac receptors owing to tissue-specific clearance by ET B receptors in vivo.British journal of pharmacology · 2005Article
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2 authors at 2 institutions in 1 country.
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Abstract
1. In this study we used ligand binding techniques to determine the affinity and selectivity of endothelin receptor agonists and antagonists in human left ventricle which expresses both ETA and ETB receptors, and compared these results with cardiovascular tissues from rat and porcine hearts. 2. The linear tripeptide antagonist, FR139317 competed for [125I]-ET-1 binding to human left ventricle with over 200,000 fold selectivity for the ETA receptor (KD ETA = 1.20 +/- 0.28 nM, KDETB = 287 +/- 93 microM). The ETA-selective non-peptide antagonist, 50235, competed with lower affinity and selectivity (KDETA = 162 +/- 61 nM, KDETB = 171 +/- 42 microM) in this tissue. BQ123 and FR139317 also showed high selectivity (greater than 20,000 fold) and affinity in rat (BQ123: KDETA = 1.18 +/- 0.16 nM, KDETB = 1370 +/- 1150 microM; FR139317: KDETA = 2.28 +/- 0.30 nM, KDETB = 292 +/- 114 microM) and pig heart (BQ123: KDETA = 0.52 +/- 0.05 nM, KDETB = 70.4 +/- 4.0 microM; FR139317: KDETA = 2.17 +/- 0.51 nM, KDETB = 47.1 +/- 5.7 microM) (n > or = 3 individuals +/- s.e.mean). 3. Although BQ3020 competed with over 1000 fold selectivity for the ETB subtype in human heart (KDETB = 1.38 +/- 0.72 nM, KDETA = 2.04 +/- 0.21 microM) the peptide inhibited only the binding of [125I]-ET-1 at concentrations greater than 100 nM in rat and porcine heart. This is in contrast to the data from the ETA-selective antagonists which indicated the presence of ETB sites in these tissues from animal hearts. 4. The peptide antagonist, BQ788, had a low, micromolar affinity (KD = 1.98 +/- 0.13 microM) using human left ventricle and no significant selectivity for the human ETB-subtype in this tissue. 5. The non-peptide ET antagonists, Ro462005 (KD = 50.3 +/- 9.5 microM) and bosentan (Ro470203; KD = 77.9 +/- 7.9 nM) competed monophasically for [125I]-ET-1 binding sites in human left ventricle. 6. The results show that the ETA antagonists, BQ123 and FR139317, are highly selective for ETA receptors in all cardiac tissues tested, whereas BQ788 has a low affinity and no selectivity in this human tissue. Further we showed that there are species differences in the binding of BQ3020 to the ETB receptors in the hearts derived from human, rat and pig.
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