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-effect curves on diastolic blood pressure (DBP). Renal and adrenal effects were assessed by plasma renin activity (PRA), aldosterone concentrations, and antagonistic concentration equivalents (n x Ki) in a radioligand rat lung receptor assay. Both drugs exerted similar substantial (> 30-fold) and long-lasting (> 2-fold 47 h after dosing) rightward shifts of the angiotensin II dose effect declining with half-lives of 15 h irbesartan and 12 h candesartan, respectively. Dose ratio - 1 versus n x Ki showed a linear relationship in Schild regression plots; both drugs increased PRA, decreased DBP, and suppressed aldosterone. The slopes of linear relationship between angiotensin antagonism (dose ratio - 1) and PRA increase were almost threefold steeper (p = 0.005) following irbesartan as compared with candesartan. The findings suggest that for the same degree of angiotensin II antagonism, irbesartan produces a greater increase in PRA than candesartan. These pharmacodynamic differences warrant further investigation and clarification.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Belz GG,Butzer R,Kober S,Mutschler Edoi
10.1097/00005344-200204000-00012subject
Has Abstractpub_date
2002-04-01 00:00:00pages
561-8issue
4eissn
0160-2446issn
1533-4023journal_volume
39pub_type
临床试验,杂志文章,随机对照试验abstract::To investigate the role of endothelin (ET) in severe hypertension, endothelial dysfunction hypercholesterolemic stroke-prone spontaneously hypertensive rats (SHRSP on a 5% cholesterol diet) were additionally fed with 1% NaCl and 0.023% nitro-L-arginine. Under these conditions, all untreated rats died within 30 days (m...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199800001-00069
更新日期:1998-01-01 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 pharmacologic properties of a novel nonpeptide endothelin (ET) receptor antagonist, S-1255 ([R]-[+]-2-[benzo(1,3)dioxol-5-yl]-6-isopropyl-4-[4-methoxyphenyl]-2H-chromene-3-carboxylic acid), was studied. [3H]S-1255 specifically bound to porcine aortic smooth muscle membranes expressing only ET(A) receptors with a K...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200104000-00014
更新日期:2001-04-01 00:00:00
abstract:BACKGROUND:The goal of this study was to determine whether an Angiotensin II receptor antagonist, candesartan, prevents myocardial fibrosis more effectively than enalapril in animals with a non-ACE pathway during the progression of congestive heart failure (CHF). METHODS AND RESULTS:Dogs were randomly assigned to one ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200406000-00016
更新日期:2004-06-01 00:00:00
abstract::In humans, three endothelin (ET) isoforms are predicted to exist by analysis of genomic DNA. However, evidence for the presence of all three mature ET peptides and their precursors remains unclear. Our aim was to identify the ET isoforms present in human heart, using radioimmunoassay (RIA) and reverse-phase high-perfo...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199322008-00009
更新日期:1993-01-01 00:00:00
abstract::Heart failure after myocardial infarction (MI) is associated with endothelial dysfunction. There is conflicting evidence on the exact nature of this endothelial dysfunction and how endothelium-dependent vasodilation is affected by angiotensin-converting enzyme inhibitor (ACE-I) therapy. Furthermore, consequences of ac...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000187175.05780.e2
更新日期:2005-12-01 00:00:00
abstract::Our recent studies have shown that the nonpeptide angiotensin II (Ang II) antagonist losartan interacts with thromboxane A2/prostaglandin H2 receptors and inhibits the thromboxane A2 (TxA2) analog U46619-induced vasoconstriction in canine coronary arteries. In this study, we further investigated whether losartan preve...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199808000-00005
更新日期:1998-08-01 00:00:00
abstract::Increased sodium absorption in the gut is one mechanism contributing to hypertensive blood pressure values. The sodium-proton-exchanger subtype 3 (NHE3) is an important mediator of intestinal sodium absorption. The compound SAR is a new specific NHE3 inhibitor with extremely low oral absorbability leading to decreased...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0000000000000336
更新日期:2016-03-01 00:00:00
abstract::We investigated the mechanism of the vasodepressor effect of endokinin A/B. An intravenous (IV) bolus of endokinin A/B (0.05-0.3 nmol/kg) dose-dependently decreased mean arterial pressure in thiobutabarbital-anesthetized rats. The magnitude of the response was unaffected by IV pretreatment with NG-nitro-L-arginine met...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000175236.41573.2a
更新日期:2005-09-01 00:00:00
abstract::Many radioligands used to study neurotransmitter receptors label multiple subtypes or multiple classes of receptors. Frequently, two subtypes or classes of receptors coexist in the same tissue and exhibit only slightly different affinities for a radioligand. A new analytical method has been developed to quantitate the...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-01-01 00:00:00
abstract::We briefly review and compare the current knowledge of growth mechanisms for the mitogenic response of endothelial cells and smooth-muscle cells to injury. For the endothelium, this focuses on the evidence that growth control involves two components: an endogenous inhibition mechanism, which can be overcome either by ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-199321001-00007
更新日期:1993-01-01 00:00:00
abstract::It has been suggested that isosorbide dinitrate (ISDN)-induced venodilation could be ascribed to preferential accumulation of the agent in venous tissues, resulting in higher concentrations of nitric oxide (NO). Here, the authors investigated whether the venodilating effect of ISDN is associated with a preferential in...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00005344-200301000-00006
更新日期:2003-01-01 00:00:00
abstract::Previous studies in which an isolated heart or in situ constant pressure preparation was used suggested a minimal role for adenosine in autoregulatory control of coronary circulation. These results, however, are controversial, and the role of adenosine in autoregulation of flow in heart is uncertain. To test the hypot...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199409000-00012
更新日期:1994-09-01 00:00:00
abstract::The effects of R 56,865, a compound with unusual calcium antagonistic properties, on altered left ventricular (LV) diastolic properties were studied during pacing-induced ischemia in dogs with coronary stenosis. Severe coronary artery stenosis was produced on both the left anterior descending (LAD) and circumflex (Cx)...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199104000-00015
更新日期:1991-04-01 00:00:00
abstract::Sickle cell disease (SCD), the most common inherited hematologic disorder in the United States and the most common single gene disorder in the world, causes substantial morbidity and mortality. The major pathobiologic processes that underlie SCD include vaso-occlusion, inflammation, procoagulant processes, hemolysis, ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e318204bb34
更新日期:2011-02-01 00:00:00
abstract::We recently found that TGF-beta increases ET-1 secretion in MDCK, a renal tubular cell line. The secretion of ET-1, by a confluent monolayer of MDCK cells grown on a filter, to the basolateral side of the epithelium was two times greater than that to the apical side. However, TGF-beta-increased ET-1 and big ET-1 secre...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199100177-00065
更新日期:1991-01-01 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 acute, 60 min blood pressure and plasma renin responses to an oral test dose of captopril given to a quietly seated patient can be used to gain information quickly on renin dependency or lack of it in a hypertensive situation. This information is verified by a baseline renin sodium profile test. These two diagnost...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-198507004-00017
更新日期:1985-01-01 00:00:00
abstract::Before the withdrawal of 2 COX-2 selective agents (COX-2s) from the market, many rheumatoid arthritis patients were using these products regularly, with disease-modifying antirheumatic agents. Clinical trials have shown benefit of COX-2s equivalent to nonselective nonsteroidal anti-inflammatory drugs (NS-NSAIDs) in rh...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200605001-00010
更新日期:2006-01-01 00:00:00
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
更新日期:2017-10-01 00:00:00
abstract:BACKGROUND:Telmisartan is an angiotensin II receptor blocker, which acts as a partial agonist of peroxisome proliferator activator receptor-γ (PPAR-γ). Because PPAR-γ initiates a variety of antiinflammatory responses, the effect on myocardial ischemia is to be elucidated. METHODS AND RESULTS:The left anterior descendi...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e3182592d7b
更新日期:2012-08-01 00:00:00
abstract::Amylin is a 37-amino acid peptide that shares considerable homology with calcitonin gene-related peptide (CGRP). Both peptides exert glycoregulatory actions and produce vasodilation of the cardiovascular system. We wished to determine if amylin exerts vasodilatory action in the perfused mesenteric arterial bed in a ma...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199512000-00012
更新日期:1995-12-01 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::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
abstract::The cardiovascular response to 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), a selective putative 5-HT1A receptor agonist, has been investigated in the rat. Comparisons were made with clonidine, a centrally acting hypotensive agent with negligible affinity for 5-HT receptors. In conscious, spontaneously hyperte...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198703000-00010
更新日期:1987-03-01 00:00:00
abstract::Ferulic acid is a simple phenolic acid commonly present in cereals. In this study, changes in heart and kidney structure and function were measured in young N(ω)-nitro-L-arginine methyl ester (L-NAME)-treated Wistar rats and 10-month-old spontaneously hypertensive rats (SHR) alone and after chronic treatment with feru...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e31827cb600
更新日期:2013-03-01 00:00:00
abstract::Cyclosporine (CsA) treatment in solid organ transplantation has represented one of the greatest advances in the past 20 years, reducing acute rejection and increasing long-term survival. However, CsA has an important side effect, producing renal vasoconstriction and systemic hypertension. The main histological finding...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-200000001-00002
更新日期:2000-01-01 00:00:00
abstract::To assess flecainide's ability to suppress ventricular fibrillation during reperfusion, we compared flecainide acetate (2 mg/kg i.v.) with saline placebo in 50 pentobarbital-anesthetized dogs undergoing proximal anterior descending coronary artery occlusion for 20 min followed by sudden release. Treatment selection wa...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1989-04-01 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::Genetic hypertension [essential hypertension (EH) in humans and spontaneous hypertension in rats (SHRs)] is associated with an altered vascular structure, expressed in resistance vessels (small arteries) as an increased media:lumen ratio. The vascular smooth muscle cells appear normal and there is no cellular hypertro...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-199219002-00006
更新日期:1992-01-01 00:00:00