Abstract:
:Candesartan is a new angiotensin II type 1 (AT 1 ) receptor blocker that produces more effective 24-h blood pressure lowering than losartan in hypertensive patients. In in vitro tissue preparations, candesartan displays insurmountable antagonism of the responses to angiotensin II. Both irbesartan and EXP-3174, the active metabolite of losartan, have also previously been described in some studies as insurmountable AT 1 -receptor blockers, whereas losartan exhibits surmountable blockade of the AT 1 -receptor. We compared the properties of candesartan, irbesartan, losartan and EXP-3174 in isolated vascular preparations of rat portal vein and rabbit aortic strips. The concentrations of the different AT 1 -receptor antagonists that were effective in these in vitro preparations were also correlated to the non-protein bound plasma concentrations obtained in clinical use. Preparations of the rabbit aorta and the rat portal vein were dissected, mounted on a force-displacement transducer and submerged in oxygenated Krebs' buffer at 37°C. The vessel strips were pre-stretched to a passive force of 5 and 20 mN for portal vein and aorta, respectively. The response to angiotensin II, measured as the mean force development in response to increasing concentrations of angiotensin II, was recorded in the absence and presence of candesartan, 0.003-10 nmol/l, irbesartan, 1-100 nmol/l, losartan, 1-100 nmol/l, and EXP-3174, 0.01-10 nmol/l, for a period of 90 min. In rabbit aortic strips, candesartan caused a non-parallel shift and suppression of the angiotensin II concentration-response curve, with complete suppression of the response to angiotensin II at a dose of candesartan of 1 nmol/l. In contrast, irbesartan, losartan and EXP-3174 all caused a parallel shift of the concentration-response curve. No suppression of the angiotensin II response was seen with losartan, while its active metabolite caused saturable suppression of the maximal response at higher concentrations. For irbesartan, some degree of suppression of the maximal response could not be excluded at the highest concentration studied. Similar concentration-response curves were obtained in rat portal vein. Data on protein binding for the different AT 1 -receptor blockers are variable in the literature. Plasma protein binding for the different AT 1 -receptor blockers was determined (in triplicate) by liquid chromatography with fluorescence detection after equilibrium dialysis (6 h) of cold drug at a concentration of 1500 nmol/l. Protein binding was high (see Table) and, for candesartan, losartan and its active metabolite EXP-3174, in accordance with previously reported levels. For irbesartan, a large discrepancy in protein binding between previously reported and the present experimental data, obtained from two different non-associated laboratories, was found. The higher plasma protein binding for irbesartan found in the present study may explain why high doses of irbesartan seem to be needed for clinical efficacy. It appears unlikely that losartan exerts any significant inhibitory effect at therapeutic plasma levels, and the main AT 1 -blocking effect observed after oral losartan is probably exerted by EXP-3174. It is concluded that AT 1 -receptor blockers differ in their ability to inhibit angiotensin II-mediated vascular contraction, and that the antagonistic characteristics are similar in vessel preparations of different origins and with different degrees of AT 1 -receptor reserve.
journal_name
Blood Pressjournal_title
Blood pressureauthors
Morsing U Brandt-Eliasson L Renberg T Abrahamsson Pdoi
10.1080/080370500439245subject
Has Abstractpub_date
2000-01-01 00:00:00pages
50-51issue
sup1eissn
0803-7051issn
1651-1999journal_volume
9pub_type
杂志文章相关文献
BLOOD PRESSURE文献大全abstract::Home blood pressure monitoring (HBPM) is an easy and standardized tool to measure blood pressure (BP) at home, which is recommended by several national and international guidelines to obtain reliable BP values. It is a useful and dependable measure of BP, which can add information to the more common and standardized m...
journal_title:Blood pressure
pub_type: 杂志文章,评审
doi:10.3109/08037051.2015.1070599
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:The most common ophthalmologic manifestation of hypertension is hypertensive retinopathy. Our study was designed to evaluate the factors that determine retinal vessel caliber in hypertensive subjects. METHODS:During a 6-month period, retinal photographs were taken of participants during a routine yearly che...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2012.645336
更新日期:2012-06-01 00:00:00
abstract:BACKGROUND:The lack of nocturnal BP fall less than 10% of the daytime, called non-dipper hypertension, is associated with increased cardiovascular morbidity and mortality. The aim of our study was to investigate atrial conduction time in patients with non-dipper hypertension using electromechanical coupling interval an...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2010.532302
更新日期:2011-02-01 00:00:00
abstract::Self-measurement of blood pressure (BP) at home is more common than 10 years ago and encouraged by current guidelines to increase patient adherence to treatment and reach the goal of target BP. The aims of this study are to evaluate the accuracy of home sphygmomanometers and to investigate behavior/knowledge of the sp...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037050701758018
更新日期:2008-01-01 00:00:00
abstract::The aim of the present study was to compare insulin sensitivity and catecholamine responses to insulin in lean, hypertensive (HT) and normotensive (NT) premenopausal women. HT (BP 149 5/99 +/- 2 mmHg, n = 14) and NT (BP 128 +/- 4/81 +/- 2 mmHg, n = 12) were matched for age (46 +/- 1 vs. 47 +/- 1 years) and body mass i...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037059509077609
更新日期:1995-09-01 00:00:00
abstract:OBJECTIVE:To investigate if young normotensive subjects with a familial history of essential hypertension (FHH) or young borderline-hypertensive (BHT) subjects have a defect endothelial function. METHODS:Fifteen young (26 +/- 4 years) healthy normotensive (115 +/- 8/71 +/- 6 mmHg) subjects with a FHH, 31 matched healt...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/080370502320779485
更新日期:2002-01-01 00:00:00
abstract::Serotonin stimulates phospholipase A(2)(PLA(2)) leading to the production of prostaglandin products, several of which are vasoconstrictors. We hypothesised that the elevated vascular responsiveness to serotonin in deoxycorticosterone acetate (DOCA)-hypertensive rats is due in part to augmented production of vasoconstr...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037059609062117
更新日期:1996-03-01 00:00:00
abstract::This 1-year, dose-titration, General Practitioner (GP) study compared efficacy, tolerability and safety of oral temocapril (10-40 mg once daily) with atenolol (25-100 mg once daily) in mild to moderate adult hypertensives (diastolic blood pressure (DBP) 95-114 mmHg). A 12-week dose-titration period, randomized 3:1 tem...
journal_title:Blood pressure
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.3109/08037059709062074
更新日期:1997-07-01 00:00:00
abstract:AIMS:(1) To evaluate the prevalence of clinic blood pressure (BP) control in a large sample of treated hypertensives followed in our hypertension clinic during the year 2000, and to compare it with our 1997 data. (2) To investigate the prevalence of left ventricular hypertrophy (LVH) according to different levels of BP...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037050213762
更新日期:2002-01-01 00:00:00
abstract::Prehypertension is associated with increased cardiovascular events. While the "tracking phenomenon" is an important longitudinal characteristic of blood pressure (BP), changes in muscle sympathetic nerve activity (MSNA) over time remain unclear. This study tested the hypothesis that MSNA tracking contributes to BP tre...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2015.1121708
更新日期:2016-06-01 00:00:00
abstract:OBJECTIVES:Continuous positive airway pressure (CPAP) improves upper airway obstruction in patients with obstructive sleep apnoea (OSA), who often are overweight-obese. Although it is thought that CPAP improves long-term blood pressure control (BP), the impact of acute and short-term CPAP use on the cardiovascular syst...
journal_title:Blood pressure
pub_type: 临床试验,杂志文章
doi:10.1080/08037051.2018.1443391
更新日期:2018-08-01 00:00:00
abstract:BACKGROUND:Abnormal left ventricular (LV) geometric patterns, particularly concentric LV hypertrophy, are associated with a greater risk of hypertensive complications. The aim of this study was to investigate the association between LV myocardial performance index (LVMPI) and aortic distensibility (AD) with different L...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2013.778006
更新日期:2013-10-01 00:00:00
abstract:AIM:Our aim was to study different levels of high blood pressure and normal blood pressure (reference) to calculate the hazard ratios (HRs) for cardiovascular and total mortality in men and women with adjustments for many covariates. METHODS:A health-screening program was offered to a population-based sample in Stockh...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037050903013881
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:High normal blood pressure (HNBP), i.e. blood pressure (BP) > or = 130/85 mmHg and <140/90 mmHg, is an important predictor of progression to established hypertension. DESIGN:The purpose of this retrospective study was the evaluation of the predictive value of ambulatory blood pressure monitoring (ABPM) for ...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037050410021414
更新日期:2004-01-01 00:00:00
abstract::One-thousand-four-hundred-and-fifty-three patients admitted to a teaching hospital, haemodynamically stable and not severely ill nor in significant pain, were interviewed within 48 h of admission and demographic data and a detailed drinking history were obtained. Supine blood pressures (BP) were recorded on the day fo...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037059709061808
更新日期:1997-03-01 00:00:00
abstract:AIM:We determined the effect of wearing clothes under the manometer's cuff on blood pressure in manual auscultatory sphygmomanometric and automatic oscillometric blood pressure measurement. METHODS:Two hundred and one subjects were examined with the auscultatory sphygmomanometric and the automatic oscillometric method...
journal_title:Blood pressure
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1080/08037050410016465
更新日期:2004-01-01 00:00:00
abstract:BACKGROUND:There are controversial results regarding the endothelial function in patients with white coat hypertension (WCH). The aim of this study was to assess endothelial function measuring nitric oxide (NO) and C-reactive protein (CRP) level in WCH and to compare those with essential hypertension (EH) and healthy s...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2011.649541
更新日期:2012-10-01 00:00:00
abstract::The reduction in blood pressure seen with the use of beta-blocking drugs was an unexpected finding. Initially there was resistance to their use as the reduction of cardiac output and increase in peripheral resistance from beta-blockade was considered an undesirable pharmacological action for a drug in the treatment of...
journal_title:Blood pressure
pub_type: 杂志文章,评审
doi:10.1080/080370501753400665
更新日期:2001-01-01 00:00:00
abstract::The purpose of the study is to assess the relative impact of lifestyle factors including physical inactivity, cigarette smoking, and alcohol intake on insulin resistance in hypertensive patients. In total, 872 hypertensive patients, of Chinese and Japanese origin, from the Stanford Asia and Pacific Program for Hyperte...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037050410004828
更新日期:2004-01-01 00:00:00
abstract::Purpose: Previous studies that evaluated the prevalence of hypertension in Nigeria were either clinic based, non-standardized or did not include out-of-clinic blood pressure (BP) measurement. Materials and Methods: We selected a rural and an urban community in one state in each of the 6 geopolitical zones of Nigeria. ...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037051.2019.1612706
更新日期:2019-08-01 00:00:00
abstract:OBJECTIVE:There is an association between exercise systolic blood pressure (SBP) and cardiovascular disease and mortality. The aim of this study was to investigate this association, with 35 years of follow-up. METHODS:Through 1972-75, 2014 healthy, middle-aged men underwent thorough medical examination and a bicycle e...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037051.2017.1291276
更新日期:2017-08-01 00:00:00
abstract::We have previously shown that the angiotensin receptor blocker valsartan is associated with a lower incidence of new-onset type 2 diabetes than that with the calcium-channel antagonist amlodipine in the treatment of hypertensive patients at high cardiovascular risk. We have now investigated the benefits of valsartan v...
journal_title:Blood pressure
pub_type: 杂志文章,随机对照试验
doi:10.1080/08037050802169644
更新日期:2008-01-01 00:00:00
abstract:BACKGROUND:Endothelial dysfunction plays a major role in erectile dysfunction (ED). Uric acid (UA) is a marker of endothelial dysfunction. We hypothesized that increased UA levels may be associated with ED and aimed to investigate whether there is a relationship between, UA and ED in hypertensive patients. METHODS:A t...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2014.933032
更新日期:2014-12-01 00:00:00
abstract::BACKGROUND AND AIM. The ratio of deceleration time to early mitral wave velocity (mitral deceleration index, MDI) has been recently shown to predict cardiovascular events more precisely than deceleration time alone in human hypertension. Data, however, about the relationship of this parameter with cardiac structure ar...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037051.2011.553926
更新日期:2011-08-01 00:00:00
abstract::The purpose: To evaluate longitudinal trends in the prevalence of hyperuricaemia and chronic kidney disease (CKD) in Czech adults with and without arterial hypertension (HT).Materials and methods: Two independent cross-sectional surveys were performed in 2006-2009 and 2015-2018, each screening involving 1% population ...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037051.2020.1763158
更新日期:2020-10-01 00:00:00
abstract::To investigate the factors responsible for the morning rise in blood pressure (BP) in obstructive sleep apnea syndrome (OSAS) we examined a group of 253 consecutive snorers or OSAS patients. On the basis of their AHI the patients were classified in four groups. BP was measured on the evening before sleep onset and on ...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.3109/08037059509077598
更新日期:1995-07-01 00:00:00
abstract:OBJECTIVE:To compare the effects of amlodipine and candesartan on oxidized low-density lipoprotein (OxLDL), conjugated dienes (CD) and baseline diene conjugation in circulating low-density lipoproteins (LDL-BDC) level during antihypertensive treatment. METHODS:Forty-nine patients with untreated mild to moderate essent...
journal_title:Blood pressure
pub_type: 杂志文章,随机对照试验
doi:10.1080/08037050601037844
更新日期:2006-01-01 00:00:00
abstract::Treatment with angiotensin-converting enzyme (ACE) inhibitors is frequently associated with persistent dry cough. This side effect is thought to be due to the non-specific action of ACE inhibitors, which, in addition to suppressing the renin-angiotensin system (RAS), leads to the accumulation of kinins, encephalins an...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/080370500439290
更新日期:2000-01-01 00:00:00
abstract::Several lines of evidence show that metabolic syndrome represents an important therapeutic challenge for the forthcoming years. This is because of the epidemic burden of this multifaceted disease, the adverse impact on cardiovascular risk, as well as the problems posed in its management. This paper will provide an up-...
journal_title:Blood pressure
pub_type: 杂志文章,评审
doi:10.1080/08037050802677695
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:Hypertension is a global health threat and major cardiovascular risk. Various risk-prediction models for incident hypertension have been developed but not many of them have studied the risk-predictive value of life style factors in combination with cardiovascular biomarkers during long-term period of over 10...
journal_title:Blood pressure
pub_type: 杂志文章
doi:10.1080/08037051.2018.1540923
更新日期:2019-02-01 00:00:00