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Abstract. 1. Regional haemodynamic responses to endothelin (ET)-1, -2 and -3 and big ET-1 (all at 500 pmol kg-1) were assessed in the same conscious Long Evans rats (n = 8) in the absence or presence of the mixed ETA-, ETB-receptor antagonist, Ro 47-0203 (bosentan; 30 mg kg-1). Sitaxentan and ambrisentan as ETA-selective antagonists and bosentan and macitentan as dual antagonists were used as representatives of each class, respectively. ETA-selective antagonism caused a dose-dependent hematocrit/hemoglobin decrease that was prevented by ETB-selective receptor antagonism.
In addition, the effect of bosentan on serum glucose and insulin levels in both mild and severely diabetic rats and its effect on insulin-induced hypoglycemia were also determined. Restraining water immersion stress was used as a model for severe stress reported to elevate plasma ET-1 level. The ETA/ETB receptor antagonist bosentan caused a parallel shift of the concentration-contraction curve to the right at all concentrations of endothelin. ETB receptor mRNA was detected by Northern blot analysis in IMA and aortic smooth muscle cells. ET-1 acts via 2 receptors, ETA and ETB. The ET-1 receptor blockers bosentan and sitaxsentan have been shown to be beneficial in patients with PAH. Bosentan blocks both ETA and ETB receptors. Sitaxsentan selectively blocks ETA receptors. Theoretically, selective ETA blockade may be associated with greater vasodilation and clearance of ET-1 by leaving the ETB receptor unblocked.
Richard et al., 1994, Role of endogenous endothelin in myocardial and coronary endothelial injury after ischaemia and reperfusion in rats: studies with bosentan, a mixed ETA-ETB antagonist., Br. J. Pharmacol. ET-1 induces mitogenesis in ovine airway smooth muscle cells via ETA and ETB receptors. Am J Physiol.
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18 Sitaxsentan (Pfizer Ltd, New Bosentan is FDA approved for the treatment of patients with pulmonary arterial hypertension (ETA and ETB, respectively). Although these receptors are present throughout the lung tissue, ETA receptors have their highest concentrations in the pulmonary vasculature and airway smooth muscle, 2015-11-06 1995-05-01 Abstract. 1. Regional haemodynamic responses to endothelin (ET)-1, -2 and -3 and big ET-1 (all at 500 pmol kg-1) were assessed in the same conscious Long Evans rats (n = 8) in the absence or presence of the mixed ETA-, ETB-receptor antagonist, Ro 47-0203 (bosentan; 30 mg kg-1).
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The most likely explanation of this finding is that ET‐1, but not ET‐2 or ET‐3, triggered a covert mesenteric vasodilator mechanism which was antagonized by bosentan. Bosentan, a dual ET A and ET B endothelin receptor antagonist, has shown to be metabolized by the hepatic cytochrome P450. The oral bioavailability is 50% and peak plasma levels are reached within 2–3 h. The purposes of this study were to assess the role of ET B receptors in mediating endothelin‐1 (ET‐1)‐induced myocardial ischaemia and oedema in rats and to study the inhibitory action of the novel non‐pep tide ET A /ET B receptor antagonist, bosentan on these actions of ET‐1 2 The nonpeptide dual-ETR antagonist bosentan is the first oral drug approved to treat pulmonary arterial hypertension. Here we report crystal structures of human endothelin ET B receptor bound to Effects of bosentan (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats.
Read "Bosentan, the mixed ETA–ETB endothelin receptor antagonist, attenuated oxidative stress after experimental myocardial ischemia and reperfusion, Molecular and Cellular Biochemistry" on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips. Effects of bosentan (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats.
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Bosentan (Actelion Pharmaceuticals Ltd, Basel, Switzerland) was given orally at a dose of 125 mg twice daily, the current recommended maintenance dose in pulmonary arterial hypertension. 18 Sitaxsentan (Pfizer Ltd, New Bosentan is FDA approved for the treatment of patients with pulmonary arterial hypertension (ETA and ETB, respectively).
bosentan, sitaxsentan, macitentan, and ambrisentan—that are either mixed endothelin ETA/ETB receptor antagonists or that display ETA selectivity have been developed for clinical use primarily in pulmonary arterial hypertension (PAH), a progressive disease without a cure.1–3 To date, a number of
Abstract. 1.
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Orally administered bosentan effectively prevents endothelin 1-induced 2003-09-01 The ETA/ETB receptor antagonist bosentan caused tor, which equally binds ET-1 and ET-3 and preferentially a parallel shift of the concentration-contraction curve to the sarafotoxin S6c. We characterized endothelin receptor sub- right at all concentrations of endothelin. Bosentan reduced the ETA mRNA expression in bosentan-treated rats although it had no effect on ET mRNA expression (Fig. 5).In situ hybridization for preproET-1 mRNAThe cellular distribution of preproET-i mRNA in the kidneys of animals from different groups was investigated by in situ hybridization using digoxigenin-laheled riboprobes.
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S. M. Gardiner , P. A. Kemp , J. E. March , and T. Bennett Department of Physiology and Pharmacology, University of Nottingham Medical School, Queen's Medical Centre.