E6877

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Emergence of smooth muscle cell endothelin B-mediated vasoconstriction in lambs with experimental congenital heart disease and increased pulmonary blood flow.

Stephen M Black et al.

Circulation, 108(13), 1646-1654 (2003-09-10)

Endothelin-1 (ET-1) has been implicated in the pathophysiology of pulmonary hypertension. In 1-month-old lambs with increased pulmonary blood flow, we have demonstrated early alterations in the ET-1 cascade. The objective of this study was to investigate the role of potential

Decreases in rat brain aquaporin-4 expression following intracerebroventricular administration of an endothelin ET B receptor agonist.

Yutaka Koyama et al.

Neuroscience letters, 469(3), 343-347 (2009-12-23)

Aquaporins (AQPs) comprise a family of water channel proteins, some of which are expressed in brain. Expressions of brain AQPs are altered after brain insults, such as ischemia and head trauma. However, little is known about the regulation of brain

Characterization of [125I]-endothelin-1 and [125I]-BQ3020 binding to rat cerebellar endothelin receptors.

P S Widdowson et al.

British journal of pharmacology, 118(8), 2126-2130 (1996-08-01)

1. We performed radioligand binding experiments on rat cerebellar homogenates using [125I]-endothelin-1 ¿[1251]-ET-1¿ and [125I]-BQ3020 to examine the pharmacology of endothelin receptors in rat brain. Saturation experiments demonstrated a single population of binding sites with high affinity for both radioligands

Solid-phase synthesis of [Ala1,3,11,15]-endothelin-1 by a modified double-coupling procedure.

J Green

International journal of peptide and protein research, 41(5), 492-498 (1993-05-01)

[Ala1,3,11,15]-Endothelin-1, a linear analogue of endothelin-1 in which alanines replace the cystine residues, has been prepared by solid-phase synthesis in approximately 17% yield. Fmoc amino acids were coupled using an economical modified double-coupling (symmetrical anhydride followed by O-benzotriazolyl ester) procedure

Characterization of two new ETB selective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart.

P Molenaar et al.

British journal of pharmacology, 107(3), 637-639 (1992-11-01)

Two new endothelin receptor radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1, were characterized in tissue sections of human right atrium and left ventricle. Both radioligands had high affinity ([125I]-BQ3020 right atrium: KD = 0.145 +/- 0.037 nM, left ventricle: KD = 0.107 +/-

Alterations in ET-1, not nitric oxide, in 1-week-old lambs with increased pulmonary blood flow.

Boaz Ovadia et al.

American journal of physiology. Heart and circulatory physiology, 284(2), H480-H490 (2002-10-26)

Altered pulmonary vascular reactivity is a source of morbidity and mortality for children with congenital heart disease and increased pulmonary blood flow. Nitric oxide (NO) and endothelin (ET)-1 are important mediators of pulmonary vascular reactivity. We hypothesize that early alterations

Tezosentan, another selective selection for pulmonary hypertension, or not?

Angela Lorts et al.

Pediatric critical care medicine : a journal of the Society of Critical Care Medicine and the World Federation of Pediatric Intensive and Critical Care Societies, 5(6), 586-588 (2004-11-13)

Endothelin and structurally related analogs distinguish between endothelin receptor subtypes.

R L Panek et al.

Biochemical and biophysical research communications, 183(2), 566-571 (1992-03-16)

The endothelin (ET) analog ET-1[1,3,11,15-Ala] was compared with ET-1, ET-2, ET-3 and sarafotoxins (SRTX) S6b and S6c for receptor binding and function. All the peptides exhibited high affinity binding and contracted rabbit pulmonary artery with near equal potency. In rat

Characterization of endothelin receptor subtypes in isolated rat renal preglomerular microvessels.

H De León et al.

Regulatory peptides, 60(1), 1-8 (1995-12-07)

Endothelin (ET) increases renal vascular resistance by constriction of post- and preglomerular vessels in the rat. However, ET receptor subtypes in renal microvessels have not been clearly defined. Radioligand binding experiments were performed in isolated arcuate and interlobular arteries as

Endothelin receptor blockade does not alter the increase in pulmonary blood flow due to oxygen ventilation in fetal lambs.

J W Winters et al.

Pediatric research, 40(1), 152-157 (1996-07-01)

At birth, pulmonary vasodilation occurs during rhythmic distension of the lungs with oxygen. Both mechanical and humoral factors are involved, including the release of vasoactive substances such as prostacyclin and endothelium-derived nitric oxide (EDNO). However, the exact mechanisms remain unclear.

Pyrogenic action of endothelin in conscious rabbit.

T Koshi et al.

Biochemical and biophysical research communications, 186(3), 1322-1326 (1992-08-14)

Injection of 0.3 nmol/kg endothelin(ET)-1 into the ear vein of conscious rabbits induced a significant increase in body temperature. ETB receptor specific agonist, namely 4-Ala-ET-1, also caused an elevation of the body temperature in a dose-dependent manner by injection into

Different distribution of endothelin receptor subtypes in pulmonary tissues revealed by the novel selective ligands BQ-123 and [Ala1,3,11,15]ET-1.

K Nakamichi et al.

Biochemical and biophysical research communications, 182(1), 144-150 (1992-01-15)

We have demonstrated the different distribution of two distinct endothelin (ET) receptor subtypes in porcine pulmonary tissues using a radioligand binding assay. The clear differentiation of the subtypes was made possible by the discovery of two compounds, BQ-123 and [Ala1,3,11,15]ET-1

Discrimination between ETA- and ETB-receptor-mediated effects of endothelin-1 and [Ala1,3,11,15]endothelin-1 by BQ-123 in the anaesthetized rat.

M Bigaud et al.

British journal of pharmacology, 107(4), 912-918 (1992-12-01)

1. The influence of BQ-123 (a selective ETA-receptor antagonist) on the haemodynamic response elicited by endothelin-1 (ET-1) and [Ala1,3,11,15]ET-1 (a selective ETB-receptor agonist) was studied in anaesthetized rats instrumented with ultrasonic Doppler flow probes on the carotid, coeliac, mesenteric, renal

Local overflow and enhanced tissue content of endothelin following myocardial ischaemia and reperfusion in the pig: modulation by L-arginine.

Q D Wang et al.

Cardiovascular research, 29(1), 44-49 (1995-01-01)

The local myocardial overflow and tissue content of endothelin-like immunoreactivity (ET-LI) during ischaemia and reperfusion as well as the coronary vascular effects of endothelin were characterised in anaesthetised pigs. Ischaemia was induced by ligation of the left anterior descending coronary

Effects of calcium entry blockers on contractions evoked by endothelin-1, [Ala3,11]endothelin-1 and [Ala1,15]endothelin-1 in rat isolated aorta.

S Topouzis et al.

British journal of pharmacology, 98(2), 669-677 (1989-10-01)

1. The aim of the present study was to examine the contractile responses evoked by the recently characterized vasoactive peptide endothelin-1 (ET-1) and by two of its structural analogues, [Ala3,11]ET-1 and [Ala1,15]ET-1 in endothelium-denuded rat isolated aorta, and also to

Production of monocyte chemoattractant protein-1 and cytokine-induced neutrophil chemoattractant-1 in rat brain is stimulated by intracerebroventricular administration of an endothelin ETB receptor agonist.

Yutaka Koyama et al.

Neuroreport, 18(12), 1275-1279 (2007-07-17)

The role of endothelin (ET)B receptors in chemokine production in the brain of rats was examined. Intracerebroventricular administration of 500 pmol/day of Ala(1,3,11,15)-ET-1, a selective ETB agonist, for 3 or 7 days increased monocyte chemoattractant protein (MCP)-1 and cytokine-induced neutrophil

[Ala1,3,11,15]endothelin-1 analogs with ETB agonistic activity.

T Saeki et al.

Biochemical and biophysical research communications, 179(1), 286-292 (1991-08-30)

A linear peptide analog of endothelin (ET)-1, [Ala1,3,11,15]ET-1 (4AlaET-1), and its truncated peptide analogs were synthesized to study the structural requirements of ET-1 for the recognition of ETs-nonselective ETB receptors. ET-1 exhibited sub-nanomolar binding to two distinct ET receptor subtypes

Vascular activities of endothelin-1 and some alanyl substituted analogues in resistance beds of the rat.

M D Randall et al.

British journal of pharmacology, 98(2), 685-699 (1989-10-01)

1. The effects of endothelin-1 and of three analogues in which alanyl residues had been substituted in place of cysteinyl residues were studied in the rat, isolated, Krebs-Henseleit-perfused mesenteric bed and the in situ, blood-perfused, mesenteric and hindquarters circulations of

Endothelin-3 mediated proliferation in wounded human umbilical vein endothelial cells.

A D Wren et al.

Biochemical and biophysical research communications, 196(1), 369-375 (1993-10-15)

An in vitro model of endothelial cell injury was used to investigate the role of endothelins and related peptides in endothelial repair. Endothelin-3 (10-100 nM) enhanced wound repair over an 18 h period by promoting proliferation, an effect not inhibited

Endothelinb receptor agonists produce pulmonary vasodilation in intact newborn lambs with pulmonary hypertension.

J Wong et al.

Journal of cardiovascular pharmacology, 25(2), 207-215 (1995-02-01)

The hemodynamic effects of endothelin-1 (ET-1) are mediated by at least two distinct receptors: ETa and ETb receptors. Recently, ETb receptor agonists (4 Ala ET-1 and IRL 1620) were developed. To investigate the role of ETb receptor activation on the

The role of endothelin and endothelin receptor subtypes in regulation of fetal pulmonary vascular tone.

J Wong et al.

Pediatric research, 35(6), 664-670 (1994-06-01)

The physiologic role of endothelin-1 (ET-1) and its receptors in regulating fetal pulmonary vascular tone is unknown. We therefore investigated the role of ET-1 and its receptors in the regulation of fetal pulmonary vascular tone using BQ 123 (an ETa

Endothelin-stimulated secretion of natriuretic peptides by rat atrial myocytes is mediated by endothelin A receptors.

G Thibault et al.

Circulation research, 74(3), 460-470 (1994-03-01)

Endothelin (ET), a potent vasoconstrictor peptide, is known to enhance the secretion of atrial natriuretic factor (ANF) by the heart. In the present study, we investigated the potency of ET isopeptides to stimulate ANF and brain natriuretic peptide (BNP) secretion

Intracerebroventricular administration of an endothelin ETB receptor agonist increases expression of tissue inhibitor of matrix metalloproteinase-1 and -3 in rat brain.

Y Koyama et al.

Neuroscience, 147(3), 620-630 (2007-06-09)

Production of tissue inhibitors of matrix metalloproteinases (TIMPs), a family of secreted proteins with inhibitory actions on matrix metalloproteinases (MMPs), is up-regulated following nerve injuries and is suggested to have protective effects against MMP-mediated tissue damages. To clarify the extracellular

Endothelins stimulate the production of stromelysin-1 in cultured rat astrocytes.

Yutaka Koyama et al.

Biochemical and biophysical research communications, 371(4), 659-663 (2008-04-29)

The effects of endothelins (ETs) on the production of stromelysins, a sub-family of matrix metalloproteinases, were examined in cultured astrocytes. The treatment of cultured rat astrocytes with ET-1 increased stromelysin-1 mRNA levels, while stromelysin-2 and -3 mRNAs were not affected.

Tezosentan, a combined parenteral endothelin receptor antagonist, produces pulmonary vasodilation in lambs with acute and chronic pulmonary hypertension.

Robert K Fitzgerald et al.

Pediatric critical care medicine : a journal of the Society of Critical Care Medicine and the World Federation of Pediatric Intensive and Critical Care Societies, 5(6), 571-577 (2004-11-09)

To investigate the hemodynamic effects of tezosentan in the intact lamb both at rest and during acute and chronic pulmonary hypertension. Prospective, randomized experimental study. University-based research laboratory. Lambs with and without pulmonary hypertension. Six newborn lambs were instrumented to

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