Cultured vascular smooth muscle cells: an in vitro system for study of alpha-adrenergic receptor coupling and regulation.

Abstract:

:Cultured vascular smooth muscle cells derived by enzymatic dissociation of rabbit aortic media were used for study of alpha 1-adrenergic receptors (AAR) and receptor-coupled calcium flux. AAR were characterized by binding of the alpha 1-selective radioligand [3H]prazosin, and norepinephrine-stimulated 45calcium efflux was measured as an index of AAR-mediated calcium flux. The binding of [3H]prazosin to a crude cellular homogenate was to a single, saturable site of high affinity (Kd = 0.15 nM, Bmax = 75-125 fmol/mg protein), which was stereo-specific and exhibited the appropriate potency order for competition by agonists. Prazosin (Kd = 0.07 nM) was approximately 3000-fold more potent than the alpha 2-selective antagonist yohimbine (Kd = 222 nM), both of which exhibited Hill coefficients of one, indicative of binding to a single receptor type. In intact cells, norepinephrine caused a concentration-related (EC50 = 100 nM) increase in 45calcium efflux which was blocked by low concentrations of prazosin (IC50 approximately equal to 0.1 nM), but not yohimbine (IC50 greater than 100 nM). An alpha 1-selective concentration of prazosin (100 nM) fully blocked norepinephrine-stimulated 45calcium efflux, and therefore, it appears that this effect does not involve alpha 2-adrenergic receptors. Treatment of cultured cells with 1-norepinephrine for 48 h caused a concentration-related decrease in both AAR density and maximum norepinephrine-stimulated 45calcium efflux. This cultured vascular smooth muscle cell system provides several advantages for the study of alpha-adrenergic receptor coupling and regulation.

journal_name

J Cardiovasc Pharmacol

authors

Colucci WS,Brock TA,Atkinson WJ,Alexander RW,Gimbrone MA Jr

subject

Has Abstract

pub_date

1985-01-01 00:00:00

pages

S79-86

eissn

0160-2446

issn

1533-4023

journal_volume

7 Suppl 6

pub_type

杂志文章
  • Vasodilation by medroxalol mediated by beta 2-adrenergic receptor stimulation.

    abstract::A contribution by active vasodilation to the hypotensive effect of medroxalol was investigated in anesthetized dogs and reserpinized pithed rats. In anesthetized dogs, intravenous doses of medroxalol, which decreased blood pressure and heart rate, also produced a dose-related vasodilation in the isolated perfused grac...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198301000-00022

    authors: Dage RC,Hsieh CP,Spedding M

    更新日期:1983-01-01 00:00:00

  • Effect of ouabain on the responses to vasoconstrictor agents in isolated perfused rat tail arteries.

    abstract::In isolated rat tail arteries perfused with Krebs-Henseleit solution, ouabain, in concentrations of less than 10(-5) M, caused a concentration-dependent, noncompetitive inhibition of the vasoconstrictor response to phenylephrine. Concentrations of 10(-8) and 10(-6) M caused 30 and 61% inhibition, respectively. The inh...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198507000-00013

    authors: Armsworth SJ,Marwood JF,Stokes GS

    更新日期:1985-07-01 00:00:00

  • Segmental regulation of sodium and water excretion by TRPV1 activation in the kidney.

    abstract::Our previous studies show that activation of the transient receptor potential vanilloid type 1 (TRPV1) channels by a selective agonist, capsaicin (CAP), given unilaterally into the renal pelvis leads to increases in urine flow rate (Uflow) and urinary sodium excretion (UNa) bilaterally, although the mechanisms underly...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0b013e318168d120

    authors: Zhu Y,Wang DH

    更新日期:2008-05-01 00:00:00

  • Felodipine is more effective than hydrochlorothiazide when added to a beta-blocker in treating elderly hypertensive patients.

    abstract::This randomized, double-blind, parallel-group study compared felodipine and hydrochlorothiazide (HCT) given in addition to a beta-blocker in 134 elderly hypertensive patients aged 56-79 years (mean of 66 +/- 5 years). In the felodipine-treated group (n = 57), supine blood pressure (BP) was reduced from 171 +/- 16/101 ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-199015004-00030

    authors: Weissel M,Stanek B,Flygt G

    更新日期:1990-01-01 00:00:00

  • Pharmacodynamic studies on the angiotensin II type 1 antagonists irbesartan and candesartan based on angiotensin II dose response in humans.

    abstract::The in vivo effects of two unsurmountable angiotensin II type 1 (AT1) antagonists, irbesartan (150 mg) and candesartan (8 mg), were studied in a double-blind, randomized, crossover study in 18 healthy men. The drugs' direct vascular effects were assessed as the rightward shift (dose ratio - 1) of angiotensin dose-effe...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-200204000-00012

    authors: Belz GG,Butzer R,Kober S,Mutschler E

    更新日期:2002-04-01 00:00:00

  • Positive inotropic effect of DPI 201-106 in spontaneously hypertensive rats: lack of inhibition by adenosine and cholinergic agents.

    abstract::The positive inotropic effect of DPI 201-106 has been studied in isolated, electrically driven papillary muscles of spontaneously hypertensive rats (SHR) and Wistar-Kyoto rats (WK). The positive inotropic effect of isoprenaline (Iso) and Ca2+ was studied for comparison. The maximal positive inotropic effect of Iso was...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198804000-00012

    authors: Böhm M,Diet F,Erdmann E

    更新日期:1988-04-01 00:00:00

  • Verapamil in the treatment of hypertension.

    abstract::A randomized, double-blind, crossover trial was carried out in 17 hypertensive patients to evaluate the hypotensive efficacy and safety of verapamil. Verapamil in doses of 120 mg thrice daily was compared with pindolol in doses of 7.5 mg twice daily. A thiazide diuretic was given with both drugs. Blood pressure fell a...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-198103000-00007

    authors: Anavekar SN,Christophidis N,Louis WJ,Doyle AE

    更新日期:1981-03-01 00:00:00

  • Electromechanical dissociation after ventricular fibrillation: prevention with calcium-entry blockers.

    abstract::Calcium-entry blockers were administered in an attempt to protect myocardium during cardiac arrest due to ventricular fibrillation in mechanically ventilated dogs. An intravenous injection of verapamil, nifedipine, or lidoflazine was administered prior to successively prolonged episodes of ventricular fibrillation, du...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Vincent JL,Goldstein J,Dufaye P,Domb M

    更新日期:1984-11-01 00:00:00

  • Red wine induced modulation of vascular function: separating the role of polyphenols, ethanol, and urates.

    abstract::By using red wine (RW), dealcoholized red wine (DARW), polyphenols-stripped red wine (PSRW), ethanol-water solution (ET), and water (W), the role of wine polyphenols, ethanol, and urate on vascular function was examined in humans (n = 9 per beverage) and on isolated rat aortic rings (n = 9). Healthy males randomly con...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1097/01.fjc.0000211762.06271.ce

    authors: Boban M,Modun D,Music I,Vukovic J,Brizic I,Salamunic I,Obad A,Palada I,Dujic Z

    更新日期:2006-05-01 00:00:00

  • Role of Fas/Fas-L in vascular cell apoptosis.

    abstract::Apoptosis of vascular cells is observed in vivo in normal vessel development and a variety of vascular pathologies. Apoptosis occurs in all cell types within the vessel wall, the consequences of which depend on both cell type and the pathology under study. The death receptor Fas is expressed throughout the vessel wall...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1097/FJC.0b013e318198fe60

    authors: Stoneman VE,Bennett MR

    更新日期:2009-02-01 00:00:00

  • The effects of ACE inhibition on progression of atherosclerosis.

    abstract::Angiotensin-converting enzyme inhibitors have been extensively studied and established in the treatment of hypertension, heart failure, and ventricular dysfunction. They have various cardiac and vascular protective effects, but the relevant mechanisms of action in these areas remain to be fully understood. Possible ef...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:

    authors: Sharpe N

    更新日期:1993-01-01 00:00:00

  • Interaction of lacidipine with its receptor binding site supports a slow onset and long duration of action.

    abstract::[3H]lacidipine binding to its receptor was characterized to explain its slow onset and long duration of antihypertensive activity. Binding parameters were studied in guinea pig myocardial and cerebral membrane preparations and compared with another dihydropyridine (DHP) calcium antagonist, isradipine. Lacidipine binds...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199602000-00017

    authors: Graziani F,Ratti E,van Amsterdam FT

    更新日期:1996-02-01 00:00:00

  • Nitrendipine reverses vasoconstriction and renal hemodynamic changes in experimental hypertension.

    abstract::Nitrendipine, a calcium entry blocker, was administered by gavage (3 mg/100 g body weight/day) to rats with prolonged angiotensin-II-(AII) induced hypertension. AII was infused by osmotic minipump implanted subcutaneously. Persistent hypertension was established after 5 days. Normotensive control rats had empty sham p...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Sterzel RB,Huelsemann JL,McKenzie DE,Wilcox CS

    更新日期:1984-01-01 00:00:00

  • Effects of long-term blood pressure control on left and right ventricular structure and function in hypertensive patients.

    abstract::The functional and anatomical abnormalities of the right ventricle may occur in hypertensive patients with left ventricular hypertrophy (LVH). The present study was designed to assess the functional and structural changes in both left and right ventricles induced by chronic antihypertensive therapy. Doppler and standa...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199117002-00039

    authors: Cuspidi C,Sampieri L,Angioni L,Boselli L,Bragato R,Leonetti G,Zanchetti A

    更新日期:1991-01-01 00:00:00

  • Is the increased responsiveness to verapamil in the forearm resistance vessels of patients with hypertension a consequence of structural change?

    abstract::A mathematical model has been developed that relates wall tension in resistance vessels to changes in both distending pressure and flow; the effect of alterations in wall: lumen ratio is taken into account. The model indicates that increased autoregulatory activity in the forearm circulation of patients with primary h...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198812006-00016

    authors: Robinson BF,Benjamin N

    更新日期:1988-01-01 00:00:00

  • Stroke as a clinical problem in hypertension.

    abstract::Stroke is a major clinical problem in hypertension. Cerebral hemorrhage has become considerably less frequent since treatment of hypertension has become more widely used. Antihypertensive treatment has also reduced the incidence of lacunar stroke, which is a result of hypertensive vascular disease of small arteries. C...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:

    authors: Doyle AE,Donnan GA

    更新日期:1990-01-01 00:00:00

  • Mibefradil-induced inhibition of proliferation of human peripheral blood mononuclear cells.

    abstract::To evaluate the role of intracellular calcium and particularly Ca2+-uptake in the initiation of lymphocyte mitogenesis, the effect of mibefradil, which blocks both L- and T-type calcium channels with a more selective blockade of T-type channels, on the proliferation of human peripheral blood mononuclear cells (PBMCs) ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199904000-00012

    authors: Lijnen P,Fagard R,Petrov V

    更新日期:1999-04-01 00:00:00

  • Mechanism of block of cardiac transient outward K+ current (I(to)) by antidepressant drugs.

    abstract::Imipramine, amitriptyline, mianserine, maprotiline, and trazodone are five widely used antidepressant drugs with different chemical structures. Imipramine and amitriptyline are tricyclics, mianserine and maprotiline are tetracyclics, and trazodone is a triazolopyridine derivative. We studied the effects of these drugs...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199810000-00004

    authors: Casis O,Sánchez-Chapula JA

    更新日期:1998-10-01 00:00:00

  • Selective antagonism of endothelin-A-receptors improves outcome in both head trauma and focal stroke in rat.

    abstract::Increased levels of endothelin (ET) have been demonstrated in the ischemic brain, and ET receptor antagonism has been shown to improve outcome in cerebral ischemia. However, no previous work has been carried out evaluating the role of ET and its antagonism in brain trauma as compared to experimental stroke. In this st...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-200036051-00104

    authors: Barone FC,Ohlstein EH,Hunter AJ,Campbell CA,Hadingham SH,Parsons AA,Yang Y,Shohami E

    更新日期:2000-11-01 00:00:00

  • ET-1 and PDGF BB induce MEK mRNA and protein expression in mesangial cells.

    abstract::To evaluate a possible mechanism for the chronic regulation of MAPK/ERK kinase-1 (MEK-1) and p42 mitogen-activated protein kinase (MAPK) we studied the long-term effects of the G-protein-coupled receptor agonist endothelin-1 (ET-1) and the protein tyrosine kinase-coupled receptor agonist platelet-derived growth factor...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Schramek H,Sorokin A,Watson RD,Dunn MJ

    更新日期:1995-01-01 00:00:00

  • Therapeutic potential of tetrahydrobiopterin for treating vascular and cardiac disease.

    abstract::Tetrahydrobiopterin is the reduced unconjugated pterin that serves as an essential cofactor for the normal enzymatic function of the aromatic amino acid hydroxylases and for the nitric oxide synthases (NOS). Its role in the latter biochemistry is being increasing appreciated, as depletion or oxidation of BH4 results i...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1097/FJC.0b013e318123f854

    authors: Moens AL,Kass DA

    更新日期:2007-09-01 00:00:00

  • Kinetic properties of the angiotensin converting enzyme inhibitor ramiprilat.

    abstract::The interaction of angiotensin converting enzyme (ACE) with ramiprilat was studied at pH 7.5 in the presence of 300 mmol/l sodium chloride with furanacryloyl-Phe-Gly-Gly as substrate. Ramiprilat inhibits ACE with a Ki value of 7 pmol/l. It is both a slow- and tight-binding inhibitor; the mode of inhibition is fully co...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1097/00005344-198706107-00005

    authors: Bünning P

    更新日期:1987-01-01 00:00:00

  • Controlled multicenter study with quinapril, hydrochlorothiazide, and combination in patients with moderate to severe hypertension.

    abstract::In an 8-week, double-blind, randomized, active-controlled, multicenter study with three parallel treatment groups, we compared the efficacy and safety of once-daily 20 mg quinapril plus 12.5 mg hydrochlorothiazide (HCTZ) with each drug as monotherapy in patients with moderate to severe hypertension. Hypertensive out-p...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,多中心研究,随机对照试验

    doi:10.1097/00005344-199507000-00018

    authors: Romero R,Castellote E,Ocón J,Wagner B

    更新日期:1995-07-01 00:00:00

  • Resolvin D1 Reduces Infarct Size Through a Phosphoinositide 3-Kinase/Protein Kinase B Mechanism.

    abstract::This study was designed to determine if Resolvin D1 (RvD1), a pro-resolution metabolite of the omega-3 polyunsaturated fatty acid docosahexaenoic acid, could decrease myocardial infarct size with delivered at the onset of ischemia. Male Sprague Dawley rats underwent 40 minutes of myocardial ischemia followed by reperf...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0000000000000245

    authors: Gilbert K,Bernier J,Bourque-Riel V,Malick M,Rousseau G

    更新日期:2015-07-01 00:00:00

  • Sodium/calcium exchange and the control of contractility in cardiac muscle and vascular smooth muscle.

    abstract::A sodium/calcium exchange mechanism that mediates both Ca2+ exit and Ca2+ entry is present in the sarcolemma of most types of muscle including mammalian cardiac muscle and vascular smooth muscle (VSM). The rate and direction of Ca2+ transport mediated by the exchanger are normally regulated primarily by: (a) the intra...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:

    authors: Blaustein MP

    更新日期:1988-01-01 00:00:00

  • Folic Acid Impairs the Uptake of 5-Methyltetrahydrofolate in Human Umbilical Vascular Endothelial Cells.

    abstract:BACKGROUND:Adequate folate status supports endothelial structure and function. Folic acid (FA), an oxidized synthetic folate, which is present in the plasma of patients consuming fortified food or FA supplements, may impair cellular uptake of physiological, reduced folates. We studied the effect of FA on uptake of the ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0000000000000514

    authors: Smith D,Hornstra J,Rocha M,Jansen G,Assaraf Y,Lasry I,Blom H,Smulders YM

    更新日期:2017-10-01 00:00:00

  • Regulatory effect of Rac1 on vascular reactivity after hemorrhagic shock in rats.

    abstract::We used isolated superior mesenteric arteries (SMAs) from hemorrhagic-shock rats and hypoxia-treated vascular smooth muscle cells (VSMCs; mimicking the shock state) to observe the effects of platelet-derived growth factor (PDGF; Rac1 stimulator) and NSC23766 (Rac1 antagonist) on vascular reactivity and the relationshi...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0b013e318215e21d

    authors: Li T,Yang G,Xu J,Zhu Y,Liu L

    更新日期:2011-06-01 00:00:00

  • Dissociation of cardiodepression from cardioprotection with calcium antagonists: diltiazem protects ischemic rat myocardium with a lower functional cost as compared with verapamil or nifedipine.

    abstract::This study was performed to determine if cardiodepression can be dissociated from cardioprotection with calcium antagonists and which one (diltiazem, nifedipine, or verapamil) can maximally protect ischemic myocardium at a given level of cardiodepression. Isolated rat hearts were subjected to 0.1, 0.5, or 1.0 microM d...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Grover GJ,Sleph PG

    更新日期:1989-08-01 00:00:00

  • Protection by the calcium antagonist tiapamil, against cardiac lymphatic enzyme leakage and arrhythmias in canine hearts during reperfusion.

    abstract::We examined the effects of tiapamil, a Ca2+ antagonist, on infarct size, lymphatic enzyme release, and arrhythmias in reperfused, ischemic canine hearts. Three-hour reperfusion of the left anterior descending coronary artery, which had been ligated for 3 h, significantly increased cardiac lymphatic release of lactate ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198601000-00015

    authors: Matsuura A,Ishihara T,Nakamura K,Himori N,Nakamura K

    更新日期:1986-01-01 00:00:00

  • Plasma endothelin-1 in hemodialysis treatment - the influence of hypertension.

    abstract::In patients on chronic hemodialysis hypotensive episodes are frequently encountered during the course of treatment and the prevalence of atherosclerosis is increased. Endothelin-1 (ET-1), an endothelium-derived peptide with vasoconstrictive and mitogenic effects on smooth muscles, is involved in vascular tone regulati...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/01.fjc.0000166215.50415.36

    authors: Stefanidis I,Wurth P,Mertens PR,Ikonomov V,Philippidis G,Golphinopoulos S,Makropoulos V,Liakopoulos V,Mann H,Heintz B

    更新日期:2004-11-01 00:00:00