Human saphenous vein contains both endothelin ETA and ETB contractile receptors

White, DG; Garratt, H; Jw, Mundin; Mj, Sumner; Vallance, P.; Is, Watts

doi:10.1016/0014-2999(94)90144-9

Cited by 49 publications

(24 citation statements)

References 14 publications

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“…However, comparative studies in vivo would indicate that both ETA and ETB receptors mediate vasoconstriction in human resistance and capacitance vessels (Haynes et al, 1995). This discrepancy may be due to the size and or type of preparation studied, as there is growing evidence in vitro to suggest the presence of vascular ETB receptors in human arteries and veins (Seo et al, 1994;White et al, 1994;Dashwood et al, 1995). We therefore may expect to see contributions of both ETA and ETB receptors in mediating ET-1-induced vasoconstriction in the human pulmonary circulation in vivo.…”

Section: Resultsmentioning

confidence: 99%

Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

McCulloch

Docherty

Morecroft

et al. 1996

British J Pharmacology

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Using wire myography, we have examined the endothelin (ET) receptor subtypes mediating vasoconstriction to ET peptides in human pulmonary resistance arteries (150–200 μm, i.d.). Cumulative concentration‐response curves to ET‐1, sarafotoxin 6c (SX6c) and ET‐3 were constructed in the presence and absence of the selective antagonists FR 139317 (ETA‐selective), BMS 182874 (ETA‐selective) and BQ‐788 (ETB‐selective). All agonists induced concentration‐dependent contractions. However, the response curves to ET‐1 were biphasic in nature. The first component demonstrated a shallow slope up to 1 nM ET‐1. Above 1 nM ET‐1 the response curve was markedly steeper. Maximum responses to ET‐3 and SX6c were the same as those to 1 nM ET‐1 and 30% of those to 0.1 μm ET‐1. The order of potency, taking 0.3 μm as a maximum concentration was SX6c > > ET‐3 > ET‐1 (pEC50 values of: 10.75 ± 0.27, 9.05 ± 0.19, 8.32 ± 0.08 respectively). Taking 1 nM ET‐1 as a maximum, the EC50 for ET‐1 was 10.08 ± 0.13 and therefore ET‐1 was equipotent to ET‐3 and SX6c over the first component of the response curve. Responses to ET‐1 up to 1 nM were resistant to the effects of the ETA receptor antagonists, FR 139317 and BMS 182874 but were inhibited by the ETB receptor antagonist, BQ‐788. Conversely, responses to ET‐1 over 1 nM were inhibited by the ETA receptor antagonists, FR 139317 and BMS 182874 but unaffected by the ETB receptor antagonist, BQ‐788. The results suggest that at concentrations up to 1 nM, responses to ET‐1 are mediated via the ETB receptor, whilst the responses to higher concentrations are mediated by ETA receptors.

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Section: Resultsmentioning

confidence: 99%

Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

McCulloch

Docherty

Morecroft

et al. 1996

British J Pharmacology

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“…The non-endogenous ETB agonist in mammals, sarafotoxin S6c, was also inactive in aorta and pulmonary artery (Maguire & Davenport, 1995). This peptide does cause vasoconstriction in some human vessels such as saphenous vein (White et al, 1994b, Maguire & Davenport, 1995, internal mammary artery (Seo et al, 1994;Maguire & Davenport, 1995) and vein (Seo et al, 1994), omental arteries and veins (Riezebos et al, 1994) and pulmonary arteries (Hay et al, 1993;Maguire & Davenport, 1995). Where responses did occur, these can be variable, for example a response was detected in saphenous vein in only about 50% (White et al, 1994) of individuals or less (Maguire & Davenport, 1995).…”

Section: In Situ Hybridizationmentioning

confidence: 99%

“…In pulmonary arteries, EC50 values have a range of 0.1-17 nM (Hay et al, 1993;Fukuroda et al, 1994; Maguire and in coronary arteries the range is 1-130 nM (Franco-Cereceda, 1989;Davenport et al, 1989b;Godfraind et al, 1993;Opgaard et al, 1994). In the internal mammary artery, EC50 values range from 4-10 nm (Costello et al, 1990;Luscher et al, 1990;Bax et al, 1993;White et al, 1994b) and 3-18 nm in the sapheneous vein (Luscher et al, 1990;Costello et al, 1990;Seo et al, 1994;Akar et al, 1994). However, whether the media of all of these vessels express ETA and ETB mRNA as well as the corresponding receptor protein has not been examined in detail.…”

Section: Introductionmentioning

confidence: 99%

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Endothelin ET_A and ET_B mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ET_A sub‐type

Davenport

O’Reilly

Kuc

1995

British J Pharmacology

149

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1 We measured the ratio of ETA and ETB sub-types in the media (containing mainly smooth muscle) of human cardiac arteries (aorta, pulmonary and coronary), internal mammary 4 A single band corresponding to the expected position for mRNA encoding the ETA receptor (299 base pairs) was found in the media in each of the five vessels (n = 3 individuals) using reversetranscriptase polymerase chain reaction assays. A single band corresponding to the ETB sub-type (428 base pairs) was also always detected. 5 35S-labelled antisense probes to ETA and ETB hybridised to the media of epicardial coronary arteries as well as intramyocardial vessels, confirming the presence of mRNA encoding both sub-types in the vascular smooth muscle of the vessel wall. 6 Although mRNA for both receptors was detected, competition binding using BQ123 demonstrated that the majority (at least 85%) of ET receptors present in smooth muscle are the ETA sub-type. These results provide further support for the hypothesis that the ETA sub-type is the receptor that must be blocked in humans to produce a beneficial vasodilatation in pathophysiological conditions where there is an increase in peptide concentration or receptor density.

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“…Regarding the endothelin-receptor subtypes of human vascular tissues, some reports have suggested that endothelin-induced contraction is predominantly mediated by ETA-receptors (19,20), but ETB-receptors or atypical endothelin receptors as mentioned above may also be involved, at least in part, in human small arteries or veins (11,12,21,22). Therefore, for further definitive pharmacological characterization of the endothelin-receptor subtypes on the human venous smooth muscle cells, we investigated the effects of BQ-123 and PD142893 on the contractions induced by some endothelin receptor agonists in isolated human saphenous vein.…”

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confidence: 99%

Pharmacological Heterogeneity of Both Endothelin ETA- and ETB-Receptors in the Human Saphenous Vein

Nishiyama

Takahara

Takao

et al. 1995

Japanese Journal of Pharmacology

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ABSTRACT-To study endothelin receptor subtypes that mediate the smooth muscle contraction of human saphenous vein, effects of some endothelin-receptor agonists and antagonists were examined. Endothelin (ET)-l and sarafotoxin 6b (S6b) elicited potent concentration-dependent contractions with similar pD2 values and similar maximal responses. Selective ETB-receptor agonists, sarafotoxin 6c (S6c) and IRL1620 (Suc-[Glu9, Ala'!'15]-endothelin-1(8-21)), also caused contractions, but their maximal responses were about one third of that of ET-1. ET-3 showed a biphasic concentration-responsecurve. An ETA-receptor an-or the combination of these two antagonists hardly affected the contractile effect of ET-1, while each of them markedly antagonized the effects of higher concentrations of ET-3 and S6b. Contractions induced by lower concentrations of ET-3 and S6b were resistant to these antagonists. The concentration-response curves for S6c and IRL1620 were not affected by BQ-123. The effect of IRL1620 was markedly inhibited by PD142893, while S6c-induced contractions were much more resistant to PD142893. These different sensitivities to antagonists suggested heterogeneity of both ETA-and ETB-receptors [ETA! (sensitive to BQ-123), ETA2 (resistant to BQ-123), ETB! (sensitive to PD142893) and ETB2 (resistant to PD142893)] in the human saphenous vein, although contractions mediated by ETB-subtypes have smaller maximal responses than those mediated by the ETA-subtypes.

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Human saphenous vein contains both endothelin ETA and ETB contractile receptors

Cited by 49 publications

References 14 publications

Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

Endothelin ET_A and ET_B mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ET_A sub‐type

Pharmacological Heterogeneity of Both Endothelin ETA- and ETB-Receptors in the Human Saphenous Vein

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Human saphenous vein contains both endothelin ETA and ETB contractile receptors

Cited by 49 publications

References 14 publications

EndothelinB receptor‐mediated contraction in human pulmonary resistance arteries

EndothelinB receptor‐mediated contraction in human pulmonary resistance arteries

Endothelin ETA and ETB mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ETA sub‐type

Pharmacological Heterogeneity of Both Endothelin ETA- and ETB-Receptors in the Human Saphenous Vein

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Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

Endothelin_B receptor‐mediated contraction in human pulmonary resistance arteries

Endothelin ET_A and ET_B mRNA and receptors expressed by smooth muscle in the human vasculature: majority of the ET_A sub‐type