ArticleBritish journal of pharmacology1990
Contractile activity of three endothelins (ET-1, ET-2 and ET-3) on the human isolated bronchus.
Article in British journal of pharmacology, 1990. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Immunomodulatory effects of macrolide antibiotics in respiratory disease: therapeutic implications for asthma and cystic fibrosis.Paediatric drugs · 2007Review
- Treatment of severe small airways disease in children with cystic fibrosis: alternatives to corticosteroids.Paediatric drugs · 2002Review
- Bosentan and the endothelin system in congestive heart failure.Clinical cardiology · 2000Review
- Contraction to big endothelin-1, big endothelin-2 and big endothelin-3, and endothelin-converting enzyme inhibition in human isolated bronchi.British journal of pharmacology · 2000Article
- Modulation of ET-1-induced contraction of human bronchi by airway epithelium-dependent nitric oxide release via ET(A) receptor activation.British journal of pharmacology · 1999Article
- The induction of a biphasic bronchospasm by the ETB agonist, IRL 1620, due to thromboxane A2 generation and endothelin-1 release in guinea-pigs.British journal of pharmacology · 1996Article
- Endothelins-induce cyclicAMP formation in the guinea-pig trachea through an ETA receptor- and cyclooxygenase-dependent mechanism.British journal of pharmacology · 1996Article
- Humoral control of airway tone.Thorax · 1996Article
- Necessity of dual blockade of endothelin ETA and ETB receptor subtypes for antagonism of endothelin-1-induced contraction in human bronchi.British journal of pharmacology · 1996Article
- Potentiation by endothelin-1 of cholinergic nerve-mediated contractions in mouse trachea via activation of ETB receptors.British journal of pharmacology · 1995Article
- High-yield production of human big endothelin-1 by a combination of chemical modification and proteolysis of a fusion protein in Escherichia coli.Applied microbiology and biotechnology · 1994Article
- Mechanical and biochemical responses to endothelin-1 and endothelin-3 in bovine bronchial smooth muscle.British journal of pharmacology · 1994Article
- Inhibitory effects of nordihydroguaiaretic acid on ETA-receptor-mediated contractions to endothelin-1 in rat trachea.British journal of pharmacology · 1994Article
- Endothelin receptor subtypes in human and guinea-pig pulmonary tissues.British journal of pharmacology · 1993Article
- Review
- Endothelin-induced contraction and mediator release in human bronchus.British journal of pharmacology · 1993Article
- Contractile activity of big endothelin-1 on the human isolated bronchus.British journal of pharmacology · 1992Article
- Phosphoramidon potentiates the contractile response to endothelin-3, but not endothelin-1 in isolated airway tissue.British journal of pharmacology · 1992Article
- Endothelin-1-induced [3H]-inositol phosphate accumulation in rat trachea.British journal of pharmacology · 1992Article
- Endothelin-1 inhibits pre-stimulated tracheal submucosal gland secretion and epithelial albumin transport.British journal of pharmacology · 1991Article
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Authors and funding
5 authors.
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Abstract
1. The effects of three endothelins: (i) the classical or human/porcine endothelin (ET-1); (ii) [Trp6, Leu7] endothelin (ET-2) and (iii) [Thr2, Phe4, Thr5, Tyr6, Lys7, Tyr14] endothelin or rat endothelin (ET-3) were tested on the human isolated bronchus. 2. ET-1 produced a concentration-dependent contraction of the human isolated bronchus that proceeded in two different steps. The first step was observed at very low concentrations (pD2 = 11.01 +/- 0.17, n = 10) but corresponded to a low intrinsic activity (Emax = 15.6 +/- 1.8% of Emax = 26.1 +/- 2.9% of ACh 3 x 10(-3) M, n = 5, P less than 0.05), reduced by nicardipine 10(-6) M (Emax = 6.0 +/- 2.6% of ACh 3 x 10(-3) M, n = 5, P less than 0.05) and strongly inhibited in calcium-free medium. The second step of the action of ET-1 corresponded to a lesser potency (pD2 = 7.90 +/- 0.17, n = 9) but a higher intrinsic activity (Emax = 82.5 +/- 4.7% of ACh 3 x 10(-3) M). This effect was not significantly modified by nicardipine 10(-6) M or by Bay K 8644 10(-7) M. Neither of the two effects was modified by indomethacin 3 x 10(-6) M. 3. The effects of ET-2 and ET-3 were qualitatively similar to those of ET-1 but quantitatively different; for these two steps of contracting activity and for potency and efficacy the ranking was: ET-1 greater than ET-2 = ET-3. 4. Thus, ET-1 appears to be the most potent of these three substances in its effect on the human isolated bronchus. Its activity seems to involve the action of voltage-dependent calcium channels at low concentrations (10-12 to 10-9M), whereas other mechanisms are involved at higher concentrations (10-8 to 3 x 10-7M).
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