Abstract:
:Intracellular pH (pHi) regulation in the heart relies on the activity of three membrane mechanisms: the Na+/H+ exchange and an Na+, HCO3(-)-dependent transport, both activated after an acid load, and the Cl-/HCO(3-) exchange, activated by an intracellular alkalinization. Whereas several specific inhibitors of Na+/H+ exchange exist, distinguishing between the two HCO3(-)-dependent mechanisms remains difficult, especially near the steady state, because of the lack of specific inhibitors. To detect one such inhibitor, we tested the effects of S20787 on pHi regulation in the rat isolated ventricular myocytes. Intracellular pH was recorded with the fluorescent probe carboxy-SNARF-1. The NH4Cl (10 mM) prepulse method was used to induce an acid load to activate the dual acid extrusion system; Cl-/HCO3- exchange was activated with the acetate (40 mM) prepulse method. Our results showed that (a) a high dose (5.10(-6) M) of S20787 did not change intracellular intrinsic buffering power, beta i; (b) the dual acid extrusion system was unaffected by S20787 in the concentration range of 10(-11)-10(-6) M; and (c) S20787 partially inhibited (approximately 50%) the activity of Cl-/HCO3- exchange in a dose-dependent manner, with an IC50 of 8.8 x 10(-10) M. This inhibitory action of S20787 did not change the steady-state pHi after 5-10 min application. Our results demonstrate that S20787 is a specific and potent partial inhibitor of Cl-/HCO3- exchange in cardiac cells.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Lagadic-Gossmann D,Le Prigent K,Baut GL,Caignard DH,Renard P,Scalbert E,Feuvray Ddoi
10.1097/00005344-199610000-00011subject
Has Abstractpub_date
1996-10-01 00:00:00pages
547-52issue
4eissn
0160-2446issn
1533-4023journal_volume
28pub_type
杂志文章abstract::Microvascular pericytes contain predominantly endothelin A (ET(A))-like binding sites and also a smaller number of ETB binding sites. In this study we verified the expression of both receptors in these cells. We then examined the effect of insulin, a potent mediator of vasodilatation, on the expression of these recept...
journal_title:Journal of cardiovascular pharmacology
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pub_type: 杂志文章,评审
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pub_type: 杂志文章,评审
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abstract::Loop diuretics could adversely influence prognosis due to activation of neurohumoral mechanism in the long term. Previous study showed torasemide, a loop diuretic with anti-aldosteronergic properties, was associated with lower mortality in patients with chronic heart failure (CHF). We evaluated the effects of torasemi...
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abstract::To investigate the effects of endothelin blockade initiated immediately after the onset of myocardial infarction on survival and left ventricular remodeling, treatment with the nonselective receptor antagonist TAK-044 (n = 22) or saline (n = 19) for 3 weeks was initiated immediately after coronary ligation in rats. Th...
journal_title:Journal of cardiovascular pharmacology
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abstract::We studied the influence of dietary L-arginine (L-ARG) supplementation on forearm resistance arteries in vivo and the effect of exogenous addition of L-ARG to subcutaneous arteries isolated from gluteal biopsies. Twenty-six healthy males were recruited, and 16 were randomly allocated in a double-blind protocol to rece...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:Journal of cardiovascular pharmacology
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更新日期:1996-05-01 00:00:00
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199507000-00013
更新日期:1995-07-01 00:00:00
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e318032aa11
更新日期:2007-04-01 00:00:00
abstract::Nebivolol is a highly selective and lipophilic beta1-adrenergic receptor antagonist with vasodilating characteristics attributed mainly to endothelial generation of nitric oxide (NO). Coincidently, rapid vascular vasodilating effects of estradiol are also widely reported and membrane-initiated signaling by estrogen re...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200405000-00005
更新日期:2004-05-01 00:00:00
abstract::The serotonin (5-HT2A) antagonistic activities and the protective effect on laurate-induced peripheral vascular lesions of AT-1015, a novel 5-HT2 receptor antagonist, were investigated. In platelet aggregation, AT-1015 selectively inhibited in vitro 5-HT2A receptor-mediated aggregation, and the activity was almost equ...
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
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更新日期:1990-01-01 00:00:00
abstract::Vasopressin secretion is stimulated by hyperosmolality, hypovolemia, or hypotension and is inhibited by hypoosmolality, hypervolemia, or hypertension. These osmotic and hemodynamic influences are mediated by neuronal afferents that originate in separate osmoreceptors or baroreceptors but ultimately converge to act on ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
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abstract:OBJECTIVE:We investigate the impact of different regimens of parenteral hydrogen sulfide (H2S) administration on myocardium during ischemia-reperfusion (IR) and the molecular pathways involved in its cytoprotective effects. METHODS:Eighteen male Yorkshire pigs underwent 60 minutes of mid-left anterior descending coron...
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abstract::The effects of endothelin-3 (ET-3) on ganglionic transmission of dog cardiac sympathetic ganglia and possible mechanisms involved were investigated in vivo and in vitro. Positive chronotropic responses to preganglionic stellate stimulation and those to dimethylphenylpiperazinium as well as McN-A-343 administered to th...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
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abstract::At present, endothelin (ET) receptor classification remains controversial. We investigated the presence of atypical ETA receptors in human saphenous veins (SV). Human SV was obtained from 24 patients undergoing coronary artery bypass grafting. Vessels were set up in organ baths, stretched to a tension of 6 g, and left...
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abstract::The combination of a beta-adrenoceptor-blocking drug with the dihydropyridine calcium channel antagonist, nitrendipine, has particular therapeutic advantages in the management of hypertension. The beta-blocker reduces any reflex increases in sympathetic nervous system and renin-angiotensin system activity that result ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199100177-00130
更新日期:1991-01-01 00:00:00
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journal_title:Journal of cardiovascular pharmacology
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journal_title:Journal of cardiovascular pharmacology
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更新日期:1984-05-01 00:00:00
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