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 activity) close to the optimum for this class of compounds.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Berntsson P,Johansson E,Westerlund Cdoi
10.1097/00005344-198710001-00011subject
Has Abstractpub_date
1987-01-01 00:00:00pages
S60-5eissn
0160-2446issn
1533-4023journal_volume
10 Suppl 1pub_type
杂志文章abstract::According to the standard model of G protein-coupled receptor (GPCR) signaling, GPCRs are localized to the cell membrane where they respond to extracellular signals. Stimulation of GPCRs leads to the activation of heterotrimeric G proteins and their intracellular signaling pathways. However, this model fails to accomm...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/FJC.0000000000000198
更新日期:2015-02-01 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::There has been some debate regarding the benefit of magnesium (Mg) in the treatment of acute myocardial infarction (AMI) because of conflicting results from recent clinical trials. Several different hypotheses have been advanced to explain the cardioprotective properties of Mg, including the influence of the timing of...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199612000-00012
更新日期:1996-12-01 00:00:00
abstract::Carvedilol is a dual-acting drug designed to produce two complementary effects: beta-blockade and vasodilation. These effects are induced in the same dose range, a prerequisite for utilizing both properties in an appropriate manner. The vasodilation is mediated predominantly by specific alpha 1-adrenoceptor blockade. ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-199219001-00003
更新日期:1992-01-01 00:00:00
abstract::The antihypertensive efficacy and tolerability of amlodipine in combination with enalapril were assessed in this two-center study. Patients with moderate to severe hypertension and with diastolic blood pressure > 95 mm Hg after 4 weeks of treatment with open-label enalapril 5-10 mg daily were randomized to receive aml...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1097/00005344-199117001-00006
更新日期:1991-01-01 00:00:00
abstract::On the basis of animal studies, it has been proposed that calcium antagonists selectively interfere with the pressor response to alpha 2-adrenoceptor antagonists and have less direct action on alpha 1-adrenoceptor mechanisms. In placebo-controlled randomized studies in healthy normotensives, we have found that verapam...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-198500076-00036
更新日期:1985-01-01 00:00:00
abstract::The peptide vasoconstrictors angiotensin II (Ang II) and endothelin-1 (ET-1), originally thought to derive exclusively from the plasma renin-angiotensin system and vascular endothelium, respectively, have been demonstrated to be produced independently of such sources. Local tissue angiotensin-generating systems are we...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-199322005-00007
更新日期:1993-01-01 00:00:00
abstract::This investigation demonstrates an increase in endothelin (ET)-mediated vascular tone in peri-ischemic areas after experimental focal cerebral ischemia (middle cerebral artery occlusion) in the cat. Adventitial application of the butenolide antagonist PD155080 (30 microM), after MCA occlusions resulted in marked incre...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-01-01 00:00:00
abstract::Calcium sensitizers increase myocardial contractile function without affecting Ca2+ homeostasis, which might be beneficial in the treatment of patients with heart failure. However, it remains uncertain whether Ca sensitizers induce quantitatively similar inotropic responses in control and failing hearts. To compare th...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200101000-00003
更新日期:2001-01-01 00:00:00
abstract::Aldosterone is increased in diabetes and contributes to the development of diabetic nephropathy. The authors hypothesized that reduction in aldosterone production in diabetes by amlodipine or aliskiren improves diabetic kidney disease by attenuating renal oxidative stress and fibrosis. Normoglycemic and streptozotocin...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e318274d2ef
更新日期:2013-01-01 00:00:00
abstract::The acute effects of daunomycin on the mechanical and energetic outputs of rabbit papillary muscles have been examined at 27 degrees C using a myothermic technique. Contrary to expectations, daunomycin, in concentrations ranging from 10 to 160 micrograms/ml, acted as a positive inotropic agent in terms of peak stress ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198505000-00023
更新日期:1985-05-01 00:00:00
abstract::Formation of oxygen free radicals during heart transplantation seems to be related to the alterations occurring during ischemia and reperfusion and could explain the short preservation time of donor hearts. The aim of our study was (a) to analyze the protective effects of pyruvate during cold cardioplegia and ischemia...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199911000-00005
更新日期:1999-11-01 00:00:00
abstract::Dimethyl sulfoxide (DMSO) is a widely used vehicle for water-insoluble substances and exerts a wide range of pharmacologic effects including anti-inflammatory and free radical scavenging properties. Additionally, in an animal model, DMSO inhibited cholesterol-induced atherosclerosis. Despite such profound pharmacologi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e3181eb3063
更新日期:2010-09-01 00:00:00
abstract::Endogenous as well as synthetic cannabinoids have potent vasodilatory actions in a variety of vascular preparations. Their precise mechanism of action is as yet unclear, but several studies point to the activation of type 1 vanilloid (TRPV1) receptors on primary afferent perivascular nerves, stimulating the release of...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000205053.53946.10
更新日期:2006-02-01 00:00:00
abstract::This study was a multicenter, double-blind comparison of the antianginal efficacy and safety of amlodipine and placebo as adjunctive therapy with constant recommended maintenance doses of beta-blockers. Patients with stable exertional angina pectoris were randomized to placebo or amlodipine at a starting dose of 5 mg ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1097/00005344-199117001-00016
更新日期:1991-01-01 00:00:00
abstract::We used strips of human pulmonary arteries from patients undergoing surgery for lung tumor to investigate whether or not this human tissue (like that of the rabbit) is endowed with inhibitory presynaptic alpha 2-adrenoceptors. The strips were incubated with [3H]noradrenaline and subsequently superfused with physiologi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198605000-00016
更新日期:1986-05-01 00:00:00
abstract::The present study examined the effects of central and peripheral administration of a vascular (V1) vasopressin (AVP) receptor antagonist on blood pressure, heart rate, and AVP levels in conscious rats. Rats subjected to rapid arterial haemorrhage were administered the AVP V1 antagonist [d(CH2)5Tyr(Me)AVP] either 5 min...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198810000-00005
更新日期:1988-10-01 00:00:00
abstract:OBJECTIVE:Genetic loci predict <5% of variation in low-density lipoprotein cholesterol (LDL-C) response to statins. Cholestanol and desmosterol are plasma markers of cholesterol absorption and synthesis, respectively. Because statins lower LDL-C by inhibiting cholesterol synthesis, we studied the relationship between c...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/FJC.0b013e3181f09bcb
更新日期:2010-10-01 00:00:00
abstract::The effects of probucol, a lipophilic antioxidant, on the myocardial dysfunction (stunning) observed during reperfusion after 15-min ischemia in rabbit heart were studied. Rabbits received food with or without 1% probucol for 3 weeks. They were then anesthetized and prepared for recording of myocardial segment shorten...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199101000-00023
更新日期:1991-01-01 00:00:00
abstract::The relationship between adrenergic nerve activity and neuronal uptake was investigated. Helically cut strips of rat tail artery were mounted in organ chambers and isometric contractions were recorded. Spontaneous contractions were occasionally observed and these contractions were blocked by phentolamine. Cumulative a...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198003000-00004
更新日期:1980-01-01 00:00:00
abstract::Disruption of atherosclerotic plaques with associated thrombus is responsible for the majority of the acute coronary syndromes. Plaque instability is related closely to the degree of inflammation. Inflammatory cells within the plaque produce cytokines that inhibit collagen production by vascular smooth muscle cells an...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:
更新日期:1998-01-01 00:00:00
abstract::Establishing the overall efficacy or safety of a drug requires a unified methodological approach and analysis of all clinical trials that are intended to be summarized. As an example, this article presents the aggregated dose-response relationship and a subgroup analysis (by age) over all studies of the antihypertensi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,meta分析
doi:10.1097/00005344-199219001-00025
更新日期:1992-01-01 00:00:00
abstract::We have recently shown that endothelin-1 (ET-1) activates two types of Ca2+-permeable nonselective cation channels (designated NSCC-1 and NSCC-2) and store-operated Ca2+ channel (SOCC). These channels can be pharmacologically discriminated using 1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1-H-imidazoe l h...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200036051-00034
更新日期:2000-11-01 00:00:00
abstract::We studied the effects of maprotiline, a tetracyclic antidepressant agent, on transmembrane potentials recorded from papillary muscles of guinea pigs and sinoatrial nodes of rabbits, using standard microelectrode techniques. Maprotiline (10-100 microM) produced dose-dependent decreases in the maximum rate of rise (Vma...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-02-01 00:00:00
abstract::Salusin-alpha and salusin-beta are newly identified bioactive peptides with hemodynamic and mitogenic activities. Recent studies have shown that salusins improve calcium uptake and protein synthesis in neonatal rat cardiomyocytes, suggesting that salusins may be regulatory factors for myocardial growth and hypertrophy...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000242059.89430.ac
更新日期:2006-08-01 00:00:00
abstract::Peripheral vascular resistance, arterial blood pressure, and left ventricular hypertrophy (LVH) are closely related. In systemic hypertension, hemodynamic changes in systolic and diastolic function accompany LVH. Both of these cardiac functions are detected with echocardiography and were measured during this study in ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:
更新日期:1994-01-01 00:00:00
abstract::We wished to determine whether pharmacologic inhibition of the exaggerated sympathetic nerve activity in congestive heart failure (CHF) could restore the renal response to exogenous atrial natriuretic peptide (ANP) administration. Left ventricular (LV) myocardial infarction was induced in Sprague-Dawley rats (n = 16) ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199011000-00013
更新日期:1990-11-01 00:00:00
abstract::This study investigated whether intrarenal endothelin-1(ET-1) contributes to sodium excretion in aged rats. Metabolic function studies were performed in male Wistar rats (3 and 24 months) treated with placebo or the orally active ET(A) receptor antagonist darusentan (20 mg/kg/d) for 4 weeks. Mean arterial pressure was...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000211709.10735.32
更新日期:2006-03-01 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::Using micropuncture techniques in euvolemic adult male Munich-Wistar rats, we assessed the functional role of renal beta-adrenoceptors in mediating neural control of glomerular filtration and proximal tubular reabsorption. The determinants of nephron filtration and rate of proximal tubular reabsorption were measured i...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199103000-00007
更新日期:1991-03-01 00:00:00