Abstract:
:We examined a relation between cyclic guanosine monophosphate (cGMP) production in thoracic aorta, as an indicator probably reflecting the vascular response, and the vascular as well as plasma levels of nicorandil administered orally to rats. Nicorandil (3 mg/kg) given orally was rapidly absorbed, reaching the maximal plasma (approximately 2,600 ng/ml) and vascular concentrations (approximately 176 ng/g) at 15 min after the dosing and thereafter decreased rapidly. Even 2 h after the dosing, the level of the vascular cGMP formation in vivo remained significantly higher (approximately 1,000 fmol/mg increase from the control level) in the nicorandil-treated group, compared with the vehicle-treated one, and was enough to develop pronounced muscle relaxation in in vitro aortic preparations. However, it seems that the vascular cGMP increase in vivo was not always correlated to the plasma concentration of nicorandil, because the plasma concentration (approximately 750 ng/ml corresponding to 3.5 microM) at 2 h after the dosing, caused only relatively low cGMP production (300-400 fmol/mg increase from the control level), when tested in in vitro aortic preparations. Our study may indicate, therefore, that the vascular cGMP elevation in vivo is due to the content of nicorandil effectively remaining at its vascular targets of action as well as the plasma nicorandil concentration.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Sakai K,Moriyasu M,Kitajima S,Akima M,Kamachi S,Tanikawa Mdoi
10.1097/00005344-199804000-00019subject
Has Abstractpub_date
1998-04-01 00:00:00pages
595-600issue
4eissn
0160-2446issn
1533-4023journal_volume
31pub_type
杂志文章abstract::Angiotensin-converting enzyme (ACE) is a widely distributed dipeptidyl carboxydipeptidase. Using computer analysis of the binding of radiolabeled ACE inhibitors, we have mapped the distribution of ACE in normal animals and in models of disease, and have studied the tissue effects of ACE inhibitors. In the myocardium, ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1991-01-01 00:00:00
abstract::The major aim of treatment of arterial hypertension is to reduce the increased risks of cardio-cerebrovascular morbidity and mortality that are associated with elevated blood pressure (BP). A direct relationship can be found between the level of BP and risk, even down to what is normally considered to be the "normoten...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1987-01-01 00:00:00
abstract::During ischemia-reperfusion an imbalance between endothelin (ET) and nitric oxide (NO) can be responsible for microcirculatory disturbances. The aim of this study was to restore the ET/NO balance to reduce the ischemia-reperfusion injury. Hepatic ischemia was induced for 30 min in 56 Wistar rats. Sham operation, ische...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200036051-00064
更新日期:2000-11-01 00:00:00
abstract::Adenosine protects the ischemic myocardium by coronary vasodilation and the depression of heart rate and contractility, improving myocardial energy balance. Adenosine effects on the myocardium are mediated predominantly by the type A1 receptors. Atrial natriuretic peptide (ANP), a vasodilator and regulator of blood vo...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199907000-00002
更新日期:1999-07-01 00:00:00
abstract::Doxorubicin (DOX), a potent antineoplastic agent, poses limitations for its therapeutic use due to the associated risk of developing cardiomyopathy and congestive heart failure. The cardiotoxicity of doxorubicin is associated with oxidative stress and apoptosis. We have recently shown that Spirulina, a blue-green alga...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000191520.48404.27
更新日期:2006-01-01 00:00:00
abstract::Besides generating renal damage, hypertension plays an important role in the progression of diabetic nephropathy. The fructose-fed rat is a well-established model both of high blood pressure and renal impairment, which is similar to diabetic nephropathy. To clarify the relationship between hypertension, glucose metabo...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000138166.34482.56
更新日期:2004-09-01 00:00:00
abstract::In addition to the hemodynamic components, the roles of various humoral factors have been emphasized in the progression of vascular and renal injury in hypertension. Radical scavenging properties have attracted much attention in this field. This article discusses the implication of antioxidant properties of the antihy...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1993-01-01 00:00:00
abstract::The disposition of amlodipine, a new calcium-channel blocker with a slow onset and long duration of action, has been investigated in humans and in the animal species used in the evaluation of drug efficacy and safety. Pharmacokinetic studies were conducted with nonlabeled drug using specific high-pressure liquid chrom...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198812007-00012
更新日期:1988-01-01 00:00:00
abstract::The equilibrating process of catecholamines (CAs) between plasma and red blood cells (RBC) was studied by measuring their erythrocyte/plasma concentration gradient (E/P ratio); ratio of E/P > 1 for a given amine was considered the consequence of its accumulation in or on RBC. We studied in vitro human blood obtained f...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199404000-00002
更新日期:1994-04-01 00:00:00
abstract::This study examined whether the adenosine potentiator, 5-aminoimidazole-4-carboxamide riboside (AICAr), could limit tissue necrosis during acute myocardial infarction in rabbit hearts with minimal coronary collateral flow. Forty-four rabbits underwent 45 min of ischemia with or without coronary reperfusion for 180 min...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199201000-00010
更新日期:1992-01-01 00:00:00
abstract::The effects on blood lipids and uric acid of six different antihypertensive drugs used alone, and of five different combinations of two antihypertensive drugs, are reported here. Prazosin significantly lowered serum low density lipoprotein and very low density lipoprotein (LDL + VLDL) cholesterol and total triglycerid...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1982-01-01 00:00:00
abstract::Oxygen-derived free radicals and their metabolites may contribute to the extension of irreversible cellular injury, which occurs on reperfusion of the previously ischemic myocardium. Therefore, therapy directed against the toxic effects of reactive oxygen species may provide protection to the ischemic myocardium, whic...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1986-09-01 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
abstract::Structural alterations after myocardial infarction (MI) in rats are usually examined only after death of the experimental animal. Magnetic resonance imaging (MRI) allows repeated and noninvasive measurements of important structural [left ventricular (LV) mass, LV wall thickness, LV chamber radius] as well as function ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199306000-00014
更新日期:1993-06-01 00:00:00
abstract::The actions of prostacyclin and its synthetic analog iloprost on the release and action of platelet-derived serotonin (5-HT) and thromboxane (TX) A2 were studied in vitro. Washed human platelet suspensions (WPS) (4 X 10(8) platelets/ml) were stimulated with arachidonic acid (AA) (30 mumol/L) and the incubate transferr...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198605000-00025
更新日期:1986-05-01 00:00:00
abstract::The present study was designed to investigate the lipid-lowering properties and mechanisms of action of a new HMG-CoA reductase inhibitor, rosuvastatin, in female ApoE*3-Leiden transgenic mice. Mice received a high fat/cholesterol (HFC) diet containing either rosuvastatin (0 [control], 0.00125%, 0.0025%, or 0.005% [w/...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200501000-00010
更新日期:2005-01-01 00:00:00
abstract::To gain insight with regard to the mode of action of calcium antagonists on the vasculature, we examined the effects of nifedipine, isradipine, felodipine, verapamil, gallopamil, and amlodipine on vasoconstrictor-induced prostacyclin synthesis in vitro. Cultured rat aortic smooth muscle cells were seeded after two to ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199004000-00012
更新日期:1990-04-01 00:00:00
abstract::Calcium entry blockers seem useful for energy conservation in the ischemic heart. Their exact mechanism of action, however, remains uncertain. In this study we investigated the effect of 30 nM nisoldipine on carbohydrate metabolism in isolated rat heart perfused with glucose-containing medium. Nisoldipine increased fl...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198505000-00013
更新日期:1985-05-01 00:00:00
abstract::Desethylamiodarone (DA) is a major metabolite of amiodarone (AM), a Class III antiarrhythmic drug. The plasma pharmacokinetics and tissue distribution of AM and DA (10 mg/kg i.v.) were compared in anesthetized dogs. Plasma, white blood cell (WBC), red blood cell (RBC), liver, and skeletal muscle samples were obtained ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198710000-00002
更新日期:1987-10-01 00:00:00
abstract::Isolated systolic hypertension (ISH) is a definite risk factor for cardiovascular complications (i.e., cardiac failure, coronary artery disease, and stroke) independent of diastolic elevation. The prevalence of ISH is estimated to be approximately 15-20% in the population above the age of 60 years, and increases with ...
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:
更新日期:1994-01-01 00:00:00
abstract:ABSTRACT:Lipid metabolism disorder and inflammatory response are considered to be the major causes of atherosclerogenesis. Astragalin, the most important functional component of flavonoid obtained from persimmon leaves, has the hypolipidemic effects. However, it is unknown, how astragalin protects against atheroscleros...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000944
更新日期:2020-10-30 00:00:00
abstract::Human saphenous veins were obtained at operation and assayed immediately (n = 10). The veins were cut into rings, suspended in organ chambers, and connected to force transducers for recording of isometric tension. One ring served as control; others were treated with either the alpha 1-adrenoceptor antagonist prazosin ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1994-03-01 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::Three-month-old spontaneously hypertensive rats were treated for 1, 2, or 3 months with daily intraperitoneal injections of naftidrofuryl (30 mg/kg). Systolic arterial pressure was measured. Tail arteries were removed and perfused at a constant flow rate of 2 ml/min. A concentration-response curve for serotonin was pr...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1990-01-01 00:00:00
abstract::In patients routinely treated with metoprolol, influences of CYP2D6 genotype on the response of heart rate to isoproterenol (IP) were studied at its peak and trough concentrations and were compared with those of bisoprolol. In 72 patients treated with metoprolol or bisoprolol, CYP2D6 genotype (ie, CYP2D6*1, *2, *4, *5...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000184117.76188.68
更新日期:2005-11-01 00:00:00
abstract::The antihypertensive effects and pharmacokinetic properties of lisinopril, an angiotensin-converting enzyme (ACE) inhibitor, were investigated in hypertensive patients with normal renal function (NRF, mean serum creatinine 1.0 mg/dl, n = 9) and those with impaired renal function (IRF, mean serum creatinine 1.7 mg/dl, ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199010000-00010
更新日期:1990-10-01 00:00:00
abstract::Cromakalim relaxes vascular smooth muscle by increasing potassium channel conductance, thus hyperpolarizing cell membranes. Its interactions in humans with the cardiovascular effects of norepinephrine, angiotensin II, and isoproterenol were investigated. Eight young normotensive male volunteers received on three diffe...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00005344-199112000-00003
更新日期:1991-12-01 00:00:00
abstract::We previously reported on the development of a pathway-selective estrogen receptor (ER) ligand, WAY-169916, that has ER-dependent antiinflammatory activity and is devoid of classic ER transcriptional activity. In the current study, WAY-169916 and 17beta-estradiol (17beta-E2) were evaluated for protective activity in m...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000211793.60528.f7
更新日期:2006-06-01 00:00:00
abstract::Protein kinase C (PKC) isoforms improve endothelial nitric oxide synthase activity and contractile Ca sensitivity in blood vessels. These actions may have opposite effects on propofol-induced vasodilation. This study examines the hypothesis that propofol induces relaxation by enhancing the PKC-mediated nitric oxide sy...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000275
更新日期:2015-09-01 00:00:00
abstract::Prostaglandins (PG) E2, E2, E2 alpha, and I2 [prostacyclin (PGI2)] were tested in vitro on collateral arteries that enlarge following chronic occlusion of the femoral artery in the dog. After contraction with an ED50 dose of KCl, serial doses of a PG were added. Collateral arteries relaxed significantly to PGI2 (10(-7...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198209000-00014
更新日期:1982-09-01 00:00:00