Abstract:
:The effects of the adrenergic antihypertensive drugs propranolol, clonidine, alpha-methyldopa, urapidil, indoramin, and prazosin on the relative rate of sterol synthesis were studied in freshly isolated human mononuclear leukocytes. Incubation of cells for 6 h in a medium containing lipid-depleted serum led to a threefold increase in the incorporation of [14C]acetate or tritiated water into sterols. (-)-Epinephrine added at zero time to the incubation medium inhibited the relative rate of sterol synthesis by 32% at a concentration of 1 mumol/L. The non-specific beta-blocker propranolol, added at equimolar concentrations, almost abolished the epinephrine-induced suppression. The beta-blocker per se had no effect on the incorporation of [14C]acetate into sterols up to a concentration of 1 mumol/l. The alpha 2-agonist clonidine and alpha-methyldopa, added in increasing concentrations at zero time, inhibited the relative rate of sterol synthesis, yielding a sigmoidal log dose-effect curve. The suppression was 43 and 24%, respectively, at a concentration of 0.1 mmol/L. The alpha 1-antagonists indoramin, prazosin, and urapidil, up to a concentration of 10 mumol/L, had no effect per se, or on the epinephrine-induced suppression of the relative synthesis rate of sterols. The results give evidence that various antihypertensive adrenergic drugs, depending on their action on beta- or alpha-adrenergic receptors, have different effects on cholesterol biosynthesis and therefore may affect cellular cholesterol homeostasis.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Krone W,Müller-Wieland D,Greten Hdoi
10.1097/00005344-198511000-00019subject
Has Abstractpub_date
1985-11-01 00:00:00pages
1134-7issue
6eissn
0160-2446issn
1533-4023journal_volume
7pub_type
杂志文章abstract::Neuropeptide Y (NPY) and ATP are considered cotransmitters with norepinephrine (NE) in sympathetic neurons innervating some blood vessels, including those of the mesentery. A prominent action of NPY is to potentiate the postjunctional contractile effect of NE as well as that of other vasoactive agents. We wished to in...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199511000-00002
更新日期:1995-11-01 00:00:00
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
更新日期:2000-11-01 00:00:00
abstract::The pharmacokinetics and dose proportionality of trandolapril, a new angiotensin-converting enzyme (ACE) inhibitor, were investigated in 12 healthy male volunteers in a four-way randomized crossover study over the therapeutic dose range, 0.5-4 mg. Trandolapril is rapidly absorbed, with a single elimination half-life (...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:1994-01-01 00:00:00
abstract::Apoptosis, a genetically controlled programmed cell death, has been found to play a role in ischemic reperfusion injury in several animal species including rats and rabbits. To examine whether this also is true for other animals, a surgically relevant model was established using an isolated in situ swine heart. Hearts...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200011000-00009
更新日期:2000-11-01 00:00:00
abstract::Several 3,5-pyridinedicarboxylic acid [4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-] esters, which are analogs to felodipine, were synthesized and tested for peroral activity and vascular selectivity. Structure-activity relationships demonstrate that felodipine has biological properties (selectivity and oral activ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198710001-00011
更新日期:1987-01-01 00:00:00
abstract::Recent studies have suggested that central nervous mechanisms are involved in the enhanced sympathetic drive observed in heart failure (HF). Nitric oxide (NO) in the brainstem has been shown to reduce sympathetic nerve activity. The aim of this study was to determine whether the expression of neuronal nitric oxide syn...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200312001-00023
更新日期:2003-12-01 00:00:00
abstract::We investigated the effects of endothelin (ET) and thrombin on the production of interleukin 6 (IL-6) in human umbilical vein endothelial cells (HUVECs). ET-1 increased IL-6 production twofold in HUVECs incubated for 18 h with 10(-10) M ET-1. Thrombin also significantly increased IL-6 production. However, stimulation ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-01-01 00:00:00
abstract::Atrial Fibrillation (AF) is accompanied by an increased risk for thromboembolic events in most affected patients. Current guidelines therefore recommend antithrombotic therapy with vitamin K antagonist (VKA) or non VKA oral anticoagulant (NOAC) in the majority of AF patients. Current AF treatment guidelines recommend ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/FJC.0000000000000297
更新日期:2015-12-01 00:00:00
abstract::Halothane opposes cardiotoxicity of neutral-sugar digitalis compounds in intact animals, presumably by depressing a sympathetic component of arrhythmogenesis. However, halothane also produces a dose-related reduction in arrhythmogenicity of ouabain in isolated canine Purkinje fibers, suggesting that the anesthetic may...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199406000-00006
更新日期:1994-06-01 00:00:00
abstract::The pharmacological characterization of a nonpeptide endothelin (ET)-receptor antagonist, PABSA [(R)-(--)-2-(benzo[1,3]dioxol-5-yl)-N-(4-isopropyl-phenylsulfon yl)-2-(6-methyl-2-propylpyridin-3-yloxy)-acetamide hydrochloride] was studied. PABSA competitively inhibited the binding of [125I]-ET-1 to A7r5 cells expressin...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199907000-00022
更新日期:1999-07-01 00:00:00
abstract::The role of delta-opioid receptors in mediating ischemic preconditioning (IPC) in rats, rabbits, and pigs has been well-established; however, no studies have been performed in dogs. Therefore, the purpose of the present study was to determine if activation of delta-opioid receptors can mimic the cardioprotective effec...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200307000-00012
更新日期:2003-07-01 00:00:00
abstract::Cardiac hypertrophy causes heart failure and is associated with hyperglycemia in patients with diabetes mellitus. Mibefradil, which acts as a T-type calcium channel blocker, exerts beneficial effects in patients with heart failure. In this study, we explored the effects and mechanism of mibefradil on high-glucose-indu...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000844
更新日期:2020-08-01 00:00:00
abstract::The comparative contributions of arachidonic acid (AA) metabolites and 5-hydroxytryptamine (5-HT) to the delay of reperfusion and rate of reocclusion after coronary thrombolysis with streptokinase were assessed in dogs using (a) single TXA2 synthase inhibition; (b) single 5-HT2-receptor blockade; (c) dual TXA2 synthas...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199301000-00009
更新日期:1993-01-01 00:00:00
abstract::A single dose of doxazosin, a long-acting postsynaptic alpha 1-adrenoceptor antagonist, was administered to seven patients with essential hypertension. Following administration of a single dose, all the patients except one who was forced to be discharged from the hospital for work, continuously received doxazosin once...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198707000-00013
更新日期:1987-07-01 00:00:00
abstract::The cardioprotective effect of angiotensin-converting enzyme (ACE) inhibitors in cardiac ischemia/reperfusion damage is assumed to result largely from inhibition of the enzymatic breakdown of endogenous bradykinin (BK). We assessed the role of nitric oxide (NO) in mediating the beneficial actions of BK and the possibl...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199503000-00014
更新日期:1995-03-01 00:00:00
abstract::Peptide 6A, a degradation of B beta chain of fibrinogen, is known to increase coronary and femoral blood flow. In this study, we examined the effects of peptide 32, an analogue of peptide 6A on coronary blood flow in anesthetized dogs. Intracoronary administration of equimolar amounts of peptide 32 and peptide 6A show...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199401000-00014
更新日期:1994-01-01 00:00:00
abstract::In strip preparations from the rabbit main pulmonary artery, it was not possible to differentiate convincingly between alpha 1- and alpha 2-adrenoceptors, when selective agonists such as methoxamine, St 587, B-HT 920, and clonidine, as well as selective antagonists such as prazosin and yohimbine were used for receptor...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1986-01-01 00:00:00
abstract::The treatment of hypertension is clearly beneficial. Blood pressure reduction with antihypertensive drugs reduces mortality and the incidence of complications such as stroke, renal failure, and congestive failure. However, analysis of long-term studies using different antihypertensive drugs indicates that the outcome ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1985-01-01 00:00:00
abstract::Hypertension is associated with dyslipidemia, which is a significant risk factor for cardiovascular complications. This study was undertaken to investigate the effects of veratric acid (VA) on blood pressure, plasma, and tissue lipid profile in N-nitro-L-arginine methyl ester (L-NAME)-induced hypertensive rats. Hypert...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e31824f9174
更新日期:2012-06-01 00:00:00
abstract::The effects of dopamine on the force of contraction and on cylic adenosine monophosphate (AMP) levels were investigated in isolated electrically driven left atria (32 degrees C, 1 Hz) and papillary muscles (37 degrees C, 0.5 Hz) of the rabbit. In both preparations only the combined application of phentolamine (10(-6) ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198009000-00007
更新日期:1980-09-01 00:00:00
abstract::Currently used antiplatelet drugs including aspirin, ticlopidine, and others are effective against certain but not all of the many endogenous platelet activators. Because of their limited efficacy, a significant number of serious thromboembolic complications still occur, highlighting the need for a more effective ther...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199803000-00016
更新日期:1998-03-01 00:00:00
abstract::The effects of the angiotensin converting enzyme (ACE) inhibitors captopril, enalapril, HOE 498, and its prodrug on reperfusion arrhythmias after 15 min of coronary ligation were investigated in the isolated rat heart. Drug concentrations were equipotent in their effect on angiotensin I pressor response. Furthermore, ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1986-07-01 00:00:00
abstract::The prevention of coronary disease in hypertensive patients will see progress in the years to come. It is clearly too much, however, to expect this progress to come exclusively from the application of new therapies, as the incidence of coronary disease in hypertensive patients depends on several factors, which are, es...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1990-01-01 00:00:00
abstract::LY53857, spiperone, ketanserin, and setoperone were potent and competitive 5-HT2-receptor antagonists in the rat jugular vein with equivalent affinities at 5-HT2 receptors. In the rat jugular vein, ritanserin blocked 5-HT2-mediated contractile responses with a depression of the maximum response in concentrations great...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-01-01 00:00:00
abstract::Chemokines are small secreted proteins with chemoattractant properties that play a key role in inflammation, metastasis, and embryonic development. We previously demonstrated a nonchemotactic role for one such chemokine pair, stromal cell-derived factor-1α and its G-protein coupled receptor, CXCR4. Stromal cell-derive...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e3181f713fe
更新日期:2010-11-01 00:00:00
abstract::The haemodynamic effects of three different methods of nitrate administration [intravenous (i.v.) isosorbide dinitrate (ISDN) and buccal and transdermal nitroglycerin (NTG)] were evaluated in 36 patients with acute left ventricular failure due to a recent myocardial infarction. Similar reductions in pulmonary artery o...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198911000-00012
更新日期:1989-11-01 00:00:00
abstract::The aim of this study was to comparatively assess the effects of irbesartan and amlodipine monotherapies on left ventricular mass index (LVMI) in patients with mild to moderate untreated hypertension and echocardiographically determined left ventricular hypertrophy (LVH). Sixty hypertensive patients (35 men, 25 women;...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-200311000-00007
更新日期:2003-11-01 00:00:00
abstract::The complex formed between endothelin (ET) and its binding protein was adequately stable to be separated by sodium dodecyl sulfate (SDS)-polyacrylamide gel electrophoresis (PAGE) at low temperature. Cross-linking was not necessary. This simple method was applied for both qualitative (determination of molecular weight ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199100177-00028
更新日期:1991-01-01 00:00:00
abstract::Imidazoline/guanidinium receptive sites (IGRS) are shown to be present in the subfornical organ and hypothalamic arcuate nucleus by a derivative of cirazoline, 2-(3-amino-4-[125I]iodophenoxy)methylimidazoline ([125I]AMIPI). Because many of the nonpeptide angiotensin II (Ang II) receptor antagonists contain imidazole r...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199609000-00012
更新日期:1996-09-01 00:00:00
abstract::Intravenous diltiazem (10-300 micrograms/kg), verapamil (10-300 micrograms/kg), nifedipine (1-100 micrograms/kg) and nicardipine (1-100 micrograms/kg) inhibited the tachycardia caused by cardiac sympathetic nerve stimulation (SNS, 0.5-4 Hz) in decentralized hearts of anesthetized dogs. The dose range of each drug requ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-10-01 00:00:00