Tissue Specificity of Endothelin Binding Sites

Bolger, Gordon T.; Liard, Francine; Krogsrud, Richard L.; Thibeault, Diane; Jaramillo, Jorge

doi:10.1097/00005344-199009000-00004

Cited by 37 publications

(11 citation statements)

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“…These studies clearly indicate the existence of functional receptors for endothelins in the bladder, which could be a promising target for the treatment of lower urinary tract symptoms. Bladder endothelin receptors have been briefly identified (3,15,16,19,20). However, bladder ET-1 receptor binding of endothelinreceptor antagonists used for the treatment of pulmonary arterial hypertension has not been examined in detail.…”

Section: Introductionmentioning

confidence: 99%

Bladder Endothelin-1 Receptor Binding of Bosentan and Ambrisentan

et al. 2014

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Section: Introductionmentioning

confidence: 99%

Bladder Endothelin-1 Receptor Binding of Bosentan and Ambrisentan

et al. 2014

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“…patients (Talartsckik et al 1990) support the possibility sf a w complex physiologic interaction between ANF and ET-1. Given the potent general smooth muscle spasmogenic properties of ET-1 (Bolger et al 1990a), and the ubiquity of ET-l binding sites (Bolger et al 1990b), it will clearly be important to further study the interactions between rANF and ET-1 in other tissues where their binding sites coexist. rather than an effect on the vasculature (Zimmerman et d. 1990).…”

Section: Resultsmentioning

confidence: 99%

“…ties, ET-1 has been found to possess vasodilatory properties in a number of vascular beds, and general smooth and cardiac muscle spasmogenic properties (Folta et al 1989;Warner et al 1989;Bolger et al 199Qa) and be a potent secretagogue in peripheral and central nervous system tissues (Fuhda et al 1988;Antunes et al 1988;Rosolowslcy and Campbell 1990;Ein et al 1990). Furthermore, high affinity binding sites that are linked to the functional effects of ET-1 are widely distributed throughout these tissues (Boussa et al 1989;Ambar et al 1989;Fabregat and Rozengurt 1990;Bolger et al 1990b).…”

Section: Introductionmentioning

confidence: 99%

Interactions between endothelin and atrial natriuretic factor in the rat aortic ring preparation

Bolger¹,

Liard²,

Krogsrud³

et al. 1991

Can. J. Physiol. Pharmacol.

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The potential interaction (s) between atrial natriuretic factor (ANF) and porcine--human endothelin (ET-1) was investigated in the endothelium-denuded rat aortic ring preparation. ET-1 produced a sustained contraction of aortic rings with an ED50 of 3.6 +/- 0.49 x 10(-9) M. Within the concentration range of 10(-9) to 10(-7) M, both rat ANF 103-126 and rat ANF 99-126 when preincubated with tissues reduced the contractile efficacy of ET-1 especially at low concentrations resulting in a small but significant rightward shift of the dose--response curve to ET-1. In contrast, at a concentration of 10(-10) M, rANF 99-126 but not rANF 103-126 produced a significant leftward shift of the dose--response curve to ET-1 and an increase in the maximal developed tension for the dose--response curve to ET-1. For tissues incubated in the absence of extracellular calcium or in the presence of the calcium channel blocker nifedipine (5 x 10(-7) M), both ANF derivatives produced a dose-dependent decrease in the maximum contraction, but no change in potency to ET-1. Addition of either rANF 103-126 or rANF 99-126 to tissues maximally contracted with ET-1 resulted in relaxation, reaching a maximum of 70%. The ED50 values for relaxation were 2.7 +/- 0.51 x 10(-8) and 3.5 +/- 0.60 +/- 10(-8) M for rANF 103-126 and rANF 99-126, respectively. ET-1 did not interact with biologically responsive and clearance receptors for ANF.(ABSTRACT TRUNCATED AT 250 WORDS)

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“…[93][94][95][96] Initially, the slow dissociation of agonist-receptor complexes was given as the explanation for the long-lasting actions of ET. 97 However, ET receptors are rapidly internalized in the presence of agonist 98 and Marsault et al 99,100 suggested that sustained ET-1-induced contractions are more likely attributed to a late intracellular signaling event rather than to slow off-rate of ET-1 from receptor. More recently, Chun et al 101,102 demonstrated that ET receptors were associated with caveolae at or near the plasma membrane, that ET-1 induced rapid ET receptor endocytosis, and that ET-1 remains intact and bound to receptors for up to 2 h after endocytosis.…”

Section: Pharmacology Of the Endothelin Peptidesmentioning

confidence: 99%