Analysis of responses to endothelins in isolated porcine blood vessels by using a novel endothelin antagonist, BQ-153

Fukuroda, Takahiro; Nishikibe, Masaru; Ohta, Yoshiko; Ihara, Masaki; Yano, Mitsuo; Ishikawa, Kiyofumi; Fukami, Tatsuki; Ikemoto, Fumihiko

doi:10.1016/0024-3205(92)90353-q

Cited by 74 publications

(53 citation statements)

References 14 publications

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“…Since then, various reports have appeared on the nature of this contractile receptor. An ET A receptor appeared to be involved in the contractile response to ET-I of the porcine coronary artery (Fukuroda et al 1992), but a non-ET A receptor, different from the ET n receptor, seemed to be involved as well (Harrison et al 1992). This contention was based on the finding that ET-3 recognized a sarafotoxin $6c (selective for the ET B receptor; Williams et al 1991) sensitive receptor, which was not recognized by ET-I, thus ruling out the ET R receptor.…”

Section: Endothefin Receptors In the Coronary Arterymentioning

confidence: 93%

Endothelin receptors in the human coronary artery, ventricle and atrium

Bax

Bruinvels

Suylen

et al. 1993

Naunyn-Schmiedeberg's Arch Pharmacol

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Summary.In the present experiments we investigated endothelin (ET) receptors in the human coronary artery, and in ventricular and atrial muscle using quantitative receptor autoradiography. These data indicate that both [125I]ET-1 and [125I] Sf6b-labeled ETA and ETB binding sites in human ventricular and atrial muscle. In the human coronary artery, both radioligands labeled ETA binding sites, but [125I] Sf6b also labeled a non-ET A, non-ETB binding site with relatively high affinity for both ET-1.

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Section: Endothefin Receptors In the Coronary Arterymentioning

confidence: 93%

Endothelin receptors in the human coronary artery, ventricle and atrium

Bax

Bruinvels

Suylen

et al. 1993

Naunyn-Schmiedeberg's Arch Pharmacol

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“…For example, initial evidence suggested that ETA receptor activation mediates the vasoconstrictor effects of the ETs whereas vasodilatation is elicited by stimulation of ETB receptors (and release of NO) located on endothelial cells (Sakurai et al, 1992;Masaki et al, 1992;Warner et al, 1993). However, subsequent studies revealed that ETB receptor activation produces contraction in several vascular smooth muscles (Fukuroda et al, 1992;Sudjarwo et al, 1993;Douglas et al, 1995) including rabbit pulmonary artery (Ihara et al, 1992b;Panek et al, 1992;LaDouceur et al, 1993;Warner et al, 1993;Fukuroda et al, 1994;Ohlstein et al, 1994a,b). Based on these and other data it has been proposed that there are two subtypes of ETB receptors: 'ETBl-like', which mediate the vasodilator effects, and 'ETB2-like' which are responsible for the vasoconstrictor activity of the ETs (Sokolovsky et al, 1992;Warner et al, 1993).…”

Section: Et3 Receptor Subtypes In Pulmonary Tissuesmentioning

confidence: 99%

Comparison of endothelin _B (ET_B) receptors in rabbit isolated pulmonary artery and bronchus

Hay

Luttmann

Beck

et al. 1996

British J Pharmacology

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1 To explore potential differences between endothelin (ET) receptors in airway versus vascular smooth muscle from the same species, the ETB receptors mediating contractions produced by ET-1, ET-3 and the selective ETB ligands, sarafotoxin S6c (S6c) and BQ-3020, in rabbit bronchus and pulmonary artery were investigated by use of peptide and non-peptide ET receptor antagonists.2 In rabbit pulmonary artery SB 209670 (10 gM), a mixed ETA/ETB receptor antagonist, was a more potent antagonist of contractions produced by S6c (pKB=7.7; n=9; P<0.05), than those elicited by ET-1 (pKB= 6.7; n = 6) or ET-3 (pKB= 6.7; n = 5). BQ-788 (10 gM), an ETB receptor antagonist, inhibited responses produced by ET-3 (pKB= 5.1; n = 8), BQ-3020 (pKB= 5.2; n = 4) or S6c (pKB= 6.2; n = 9; P<0.05 compared to potency versus ET-3-or BQ-3020-induced contractions), but was without inhibitory effect on ET-1-induced contractions (n = 5). RES-701 (10 gM), another selective ETB receptor antagonist, was without effect on contractions produced by S6c (n = 4) or ET-l (n = 4), and potentiated ET-3-(n = 5) or BQ-3020-induced responses (n = 4).3 The combination of BQ-788 (10 gM) and BQ-123 (10 gM), an ETA-selective receptor antagonist, antagonized contractions produced by lower concentrations of ET-l (1 and 3 nM) in rabbit pulmonary artery, but was without effect on responses elicited by higher concentrations of ET-1 (n = 5). The combination of RES-701 (10 gM) and BQ-123 (10 gM) potentiated responses elicited by ET-1, producing a 3.7 fold shift to the left in the agonist concentration-response curve (n = 5).4 In rabbit bronchus SB 209670 (3 gM) had similar potency for antagonism of contractions produced by ET-1 (pKB=6.3; n=6), ET-3 (pKB=6.5; n=6) or S6c (pKB=6.1; n=8). BQ-788 (3 gM) was without effect on responses elicited by ET-1, ET-3 or S6c (n=6) but antagonized BQ-3020-induced contractions (pKB=6.4; n=4). RES-701 (3 gM) was without effect on contractions produced by S6c (n=6) or BQ-3020 (n=4), and potentiated rather than antagonized ET-1-or ET-3-induced responses (n=6), reflected by a significant (about 6 fold) shift to the left in ET-l or ET-3 concentration-response curves. The combination of BQ-788 (3 gM) and BQ-123 (3 gM) was without effect on contractions produced by ET-1 in rabbit bronchus (n=6). The combination of RES-701 (3 gM) and BQ-123 (3 gM) potentiated responses elicited by ET-1, producing a 5.2 fold shift to the left in the agonist concentration-response curve (n = 5).5 BQ-123 (3 or 10 gM), an ETA-selective receptor antagonist, was without effect on ET-1, ET-3 or S6c concentration-response curves (n=3-6) in rabbit pulmonary artery or rabbit bronchus. 6 These data indicate that contractions induced by ET-1, ET-3, S6c and BQ-3020 in rabbit pulmonary artery or rabbit bronchus appear to be mediated predominantly via stimulation of ETB receptors. However, the qualitative and quantitative differences in the relative profiles of the various structurally diverse peptide and non-peptide antagonists examined suggests that responses produced by th...

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“…In intact vascular strips, activation of the ETA receptor on vascular smooth muscle cells (Arai et al, 1990) induces vasoconstriction whereas activation of the ETB receptor on vascular endothelial cells (Sakurai et al, 1990) releases endotheliumderived relaxing factor, resulting in vasorelaxation (Ushio- Fukai et al, 1992). However, using BQ-123, a selective antagonist for the ETA receptor subtype (Ihara et al, 1992), it was found that non-ETA (probably ETB) receptors might also mediate vasoconstriction. These reports raise questions as to which receptor subtypes are actually involved in ET-1 and ET-3-induced contractions in the coronary artery of the pig.…”

Section: Introductionmentioning

confidence: 99%

Endothelin‐1 and endothelin‐3 regulate differently vasoconstrictor responses of smooth muscle of the porcine coronary artery

Ushio‐Fukai

Nishimura

Kobayashi

et al. 1995

British J Pharmacology

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1 Using front-surface fluorometry of fura-2 and medial strips of the porcine coronary artery, we investigated mechanisms by which endothelin-1 (ET-1) and ET-3 function as vasoconstrictors.2 In the presence of extracellular Ca2"(1.25 mM), ET-1 (10-10-7 M) increased cytosolic Ca2" concentrations ([Ca2 'a] (3) That both ET-1-and ET-3-induced contractions seem to be mediated via ETA-receptors in porcine coronary artery, and that the ETA-receptor-mediated effects of ET-1 and ET-3 can be dissociated at the sub-receptor levels of the signal transduction pathway.

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Analysis of responses to endothelins in isolated porcine blood vessels by using a novel endothelin antagonist, BQ-153

Cited by 74 publications

References 14 publications

Endothelin receptors in the human coronary artery, ventricle and atrium

Endothelin receptors in the human coronary artery, ventricle and atrium

Comparison of endothelin _B (ET_B) receptors in rabbit isolated pulmonary artery and bronchus

Endothelin‐1 and endothelin‐3 regulate differently vasoconstrictor responses of smooth muscle of the porcine coronary artery

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Analysis of responses to endothelins in isolated porcine blood vessels by using a novel endothelin antagonist, BQ-153

Cited by 74 publications

References 14 publications

Endothelin receptors in the human coronary artery, ventricle and atrium

Endothelin receptors in the human coronary artery, ventricle and atrium

Comparison of endothelin B (ETB) receptors in rabbit isolated pulmonary artery and bronchus

Endothelin‐1 and endothelin‐3 regulate differently vasoconstrictor responses of smooth muscle of the porcine coronary artery

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Comparison of endothelin _B (ET_B) receptors in rabbit isolated pulmonary artery and bronchus