Abstract:
:Myocardial alpha 1-adrenoceptor number has been reported to increase during ischaemia in myocytes consequent to an increase in acyl carnitine levels. We investigated whether this phenomenon occurs in vivo and whether the novel antiischaemic agent ranolazine will protect against it. Thirty-minute occlusion of the left anterior descending coronary artery (LAD) in anaesthetised rats produced an approximate doubling of the left ventricular (LV) alpha 1-adrenoceptor population. The carnitine palmitoyl transferase 1 (CPT1) inhibitor sodium 2-[5-(4-chlorophenyl)-pentylene]oxiran-2-carboxylate (POCA 100 micrograms/kg) reduced this ischaemia-induced increase when administered intraperitoneally (i.p.) 15 min before ischaemia and abolished the increase when administered intravenously (i.v.). The CPT1 inhibitor sodium 2-tetradecyl oxirane carboxylate dihydrate (TGDA) (500 micrograms/kg) inhibited the upregulation when administered i.p. and significantly decreased alpha 1-adrenoceptor density when administered i.v.; however, this agent, unlike POCA, reduced [3H]-prazosin binding directly. The alpha 1-adrenoceptor antagonist prazosin (100 micrograms/kg i.v.) did not prevent the increase. Direct addition of palmitoyl carnitine (10 microM) to membranes from nonischaemic myocardium caused a doubling in alpha 1-adrenoceptor number, and this effect was selective for heart membranes as compared with cerebral cortex; beta-adrenoceptor number was not modified. Ranolazine (500 micrograms/kg) inhibited upregulation when administered 15 min i.v. before ischaemia or after 3-day twice-daily (b.i.d.) i.p. pretreatment. This drug did not inhibit CPT1 directly.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Allely MC,Brown CM,Kenny BA,Kilpatrick AT,Martin A,Spedding Mdoi
10.1097/00005344-199306000-00004subject
Has Abstractpub_date
1993-06-01 00:00:00pages
869-73issue
6eissn
0160-2446issn
1533-4023journal_volume
21pub_type
杂志文章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::There is no systematic study in which the effects of vasoactive substances were investigated on pulmonary vascular resistance (PVR) in in vivo mouse by directly measuring cardiac output and the inflow and outflow pressures in the pulmonary circulation. We determined the responses of PVR, total peripheral resistance (T...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000199
更新日期:2015-04-01 00:00:00
abstract::The present study, undertaken in general practice, was designed to evaluate the effects of age on the pharmacodynamics and pharmacokinetics of a conventional and a slow-release formulation (Securon SR) of verapamil. Two groups of 12 patients with essential hypertension were treated in an open, randomized, crossover st...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-198900134-00017
更新日期:1989-01-01 00:00:00
abstract::Cicletanine, a furopyridine-derivative drug, was shown to enhance the production of endogenous prostacyclin. The potent vasodilating properties of prostacyclin are used to treat severe primary pulmonary hypertension. Prostacyclin has a short half-life and can be administered only as an i.v. infusion. The aim of this s...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-199803000-00006
更新日期:1998-03-01 00:00:00
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...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1097/FJC.0b013e3181a717f7
更新日期:2009-06-01 00:00:00
abstract::The in vivo renal microvascular effects of three antihypertensive drugs: nitrendipine, a calcium entry blocker, and two direct-acting vasodilator agents, hydralazine and minoxidil, were compared. The dilator responses of pre- and postglomerular vessels were directly observed after the topical or intravenous administra...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1987-01-01 00:00:00
abstract::Since the end of 1976 ten orally active converting enzyme inhibitors [SQ 14,225 (captopril), MK 421 (enalapril), MK 422, MK 521 (lysinopril), RHC 3659, CGS 13945, CGS 13928C, CGS 14824A, Hoe 498, S 9490-3, and Ro 31-2848] have been evaluated by our group in normal volunteers. Their ability to blunt the pressor respons...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-198507001-00002
更新日期:1985-01-01 00:00:00
abstract::Proliferation of medial smooth muscle cells (SMC) plays a major role in restenosis after coronary angioplasty and can be inhibited by heparin. Platelets stimulate SMC proliferation, and their aggregation after angioplasty can be reduced by the direct thrombin inhibitor hirudin. In a porcine coronary stent-angioplasty ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199610000-00001
更新日期:1996-10-01 00:00:00
abstract::As a receptor for transforming growth factor-β, nodal and activin, activin receptor-like kinase 7 (ALK7) previously acts as a suppressor of tumorigenesis and metastasis, which has emerged to play a key role in cardiovascular diseases. However, the potential effect and molecular mechanism of ALK7 on vascular smooth mus...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000857
更新日期:2020-08-01 00:00:00
abstract::Qian Yang He Ji (QYHJ) is a traditional Chinese medicine composed of Digitalis purpurea, Uncaria gambir, Fructus tribuli terrestris, and Ligustrum lucidum. Here, we explored whether combining an antihypertensive angiotensin II receptor blocker (ARB) therapy with QYHJ can improve the arterial functionality of hypertens...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1097/FJC.0b013e31827afddf
更新日期:2013-05-01 00:00:00
abstract::Six elderly male (65-75 years), seven elderly female (64-88 years), 15 young male (22-38 years), and nine young female (25-37 years) volunteers, all of normal body weight and clinically without cardiac or renal dysfunction, received a single 25-mg intravenous dose of lidocaine. Plasma concentrations of lidocaine were ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198311000-00027
更新日期:1983-11-01 00:00:00
abstract::The cardiovascular properties of Ro 13-6438 (R-6-chloro-1,5-dihydro-3- methylimidazo -[2,1-b] quinazolin -2[ 3H]-one), a novel nonglycoside , noncatechol cardiotonic agent, were investigated in vitro and in vivo by both intravenous and oral administration. Ro 13-6438 increased tension development of isolated guinea pi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198405000-00021
更新日期:1984-05-01 00:00:00
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 three...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198511000-00019
更新日期:1985-11-01 00:00:00
abstract::This study assessed the possible local nociceptive and hyperalgesic properties of endothelin-1 (ET-1) in the rat knee-joint incapacitation test, in which animals are placed for 1 min/h on a revolving (3 rpm) metal cylinder and nociception is measured as the time the hindpaw of the injected limb was off the cylinder (i...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199800001-00149
更新日期:1998-01-01 00:00:00
abstract::Doxazosin has been shown to lower serum cholesterol levels in the cholesterol-fed (0.75% in a synthetic diet that contains sucrose and cholic acid) C57BR/cdJ mouse. These studies show that the drug's main effect is to lower low-density lipoprotein (LDL) cholesterol and leave high-density lipoprotein (HDL) cholesterol ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198900132-00004
更新日期:1989-01-01 00:00:00
abstract::Arterial vascular resistance is established by myogenic mechanisms and is modulated both by local factors such as vasodilator metabolites and by remote controls of neurogenic and hormonal origin. This paper reports on the effects of felodipine and hydralazine on the myogenic tone and the neurogenic control of the vasc...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198710001-00019
更新日期:1987-01-01 00:00:00
abstract::Carvedilol (20 mg/kg, bid) or vehicle was given to rats surviving a myocardial infarction (MI) 24 h (n = 409). In rats with large MI, carvedilol partially preserved left ventricular (LV) function and intrinsic myocardial contractility and reactivity to beta-adrenergic stimulation. Carvedilol led to scar thickening, in...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200201000-00009
更新日期:2002-01-01 00:00:00
abstract::Fifteen patients with stable angina participated in a 12-week crossover study to evaluate the efficacy of nifedipine and nitroglycerin patches. There was an initial 2-week drug washout period followed by a 2-week control period when patients received no other antianginal treatment other than sublingual nitroglycerin f...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-198709000-00010
更新日期:1987-09-01 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::The present study has been designed to explore the beneficial effect of rosiglitazone, a peroxisome proliferator activated receptor-gamma agonist, in hyperhomocysteinemia-induced cardiac hypertrophy in rats. The hyperhomocysteinemia was induced in rats by feeding L-methionine (1.7 g/kg per day orally) for 8 weeks. The...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e3181de308b
更新日期:2010-07-01 00:00:00
abstract::Beta-adrenergic-blocking drugs (BABs) have a firm place in the therapy of cardiovascular conditions including angina and hypertension. Although all BABs are competitive inhibitors of beta-receptors, they may differ in their additional pharmacodynamics, i.e., beta1-(cardio)selectivity, partial agonistic activity (PAA),...
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::Recently, we provided in vitro and in vivo evidence that several vastatins with different potencies decrease arterial smooth-muscle cell (SMC) proliferation independently of their hypocholesterolemic properties. In this study, the in vivo dose-dependent antiproliferative activity of fluvastatin on neointimal formation...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-01-01 00:00:00
abstract::Prostaglandin E1 (PGE1) has been reported to be a coronary vasodilator and has been considered clinically in the treatment of coronary vasospasm, but its mechanism of action is not known. To evaluate the vasomotor effect of PGE1, epicardial coronary and distal resistance vessel responses were compared by PGE1 and nitr...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198908000-00012
更新日期:1989-08-01 00:00:00
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::Diabetes and CYP2C19 loss of function (LOF) alleles are associated with the variable antiplatelet activity of the prodrug clopidogrel. We conducted a randomized trial (NCT03613857) to compare the combined and individualized effects of diabetes and CYP2C19 polymorphisms on the antiplatelet reactivity of clopidogrel ver...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000881
更新日期:2020-10-01 00:00:00
abstract::During myocardial ischemia, the extracellular potassium concentration increases in a triphasic pattern, an initial early increase, a constant phase, and a late increasing phase. The aim of this study was to determine whether diltiazem inhibits the late increasing phase by maintaining glycolytic adenosine triphosphate ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199710000-00004
更新日期:1997-10-01 00:00:00
abstract::The development of numerous types of cardiovascular disease is associated with alteration of the vascular smooth muscle cell (SMC) phenotype. We have previously shown that abdominal aortic aneurysm progression in a mouse model of the disease is associated with reduced differentiation of SMCs within the lesion and that...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000395
更新日期:2016-08-01 00:00:00
abstract::Acute myocardial infarction (AMI) is known to alter the pharmacokinetics of several antiarrhythmic agents. To study the effects of AMI on the kinetics of mexiletine (MEX), a single intravenous dose of 200 mg MEX HCl was infused over 30 min in 11 patients with AMI. The study was performed within 24 h of the onset of pa...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1984-01-01 00:00:00
abstract::MCI-154 is a potent nonglycoside and non-sympathomimetic cardiotonic agent with a pyridazinone structure. We assessed its cardiac and coronary vasodilator effects by use of isolated, blood-perfused papillary muscle, sinoatrial (SA) node, and atrioventricular (AV) node preparations of dogs. The drug (1-100 nmol) was in...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198712000-00013
更新日期:1987-12-01 00:00:00
abstract::The effect of chronic inhibition of nitric oxide (NO) synthesis by NG-nitro-L-arginine methyl ester (L-NAME) on cutaneous ear blood flow (EBF) in the rabbit was examined in vivo with use of laser Doppler flowmetry. Additionally, the efficacy of inhibition of NO by L-NAME was studied ex vivo in isolated preparations of...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199308000-00017
更新日期:1993-08-01 00:00:00