Abstract:
:The relationships between the effects on blood pressure and vascular responsiveness, and the whole blood concentration of the antihypertensive drug trimazosin and its major metabolite were investigated in six normotensive male volunteers following 100 mg i.v. and 200 mg p.o. administration. Pressor responses to intravenous phenylephrine and angiotensin II were evaluated 1-3 (early) and 5-7 h (late) after drug or vehicle administration. There was a fall in blood pressure in the erect position (maximum between 4 and 8 h) associated with a modest increase in heart rate. Following treatment with trimazosin, blood pressure fell to 100/63 mm Hg with intravenous administration and 92/63 mm Hg with oral treatment, compared with the placebo value of 114/83 mm Hg. Both oral and intravenous trimazosin caused a significant rightward shift of the phenylephrine pressor dose-response curve (p less than 0.05). There was no significant shift of the angiotensin II pressor dose responses. Using linear regression analysis, the concentration of trimazosin in whole blood showed a significant correlation with the dose ratios from the phenylephrine pressor dose responses following treatment with both intravenous (r = 0.73, p less than 0.02) and oral (r = 0.57, p less than 0.05) trimazosin. There was no such correlation using dose ratios from angiotensin II pressor dose responses. There was no correlation between the concentration of the metabolite 1-hydroxytrimazosin and dose ratios from either phenylephrine or angiotensin II pressor dose responses. These observations suggest that the predominant mechanism of action of trimazosin, at doses that reduce blood pressure in humans, is through blockade of peripheral postjunctional alpha 1-adrenoceptors.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Vincent J,Elliott HL,Meredith PA,Reid JLdoi
10.1097/00005344-198509000-00015subject
Has Abstractpub_date
1985-09-01 00:00:00pages
913-8issue
5eissn
0160-2446issn
1533-4023journal_volume
7pub_type
临床试验,杂志文章,随机对照试验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 electrophysiologic effects of acutely and chronically administered amiodarone on canine Purkinje fibers were assessed using microelectrode techniques to record intracellular action potentials. Chronically treated dogs received amiodarone for 3 weeks (serum levels, 0.91 +/- 0.09 microgram/ml or 1.42 X 10(-6) M). Ac...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1989-05-01 00:00:00
abstract::Mesenteric resistance arteries (internal diameter 174-337 microns) from rats, rabbits, pigs, and humans were isolated and mounted in a myograph. In all preparations, phenylephrine (alpha 1-adrenoceptor agonist) evoked concentration-dependent contractions that were antagonized by prazosin (alpha 1-adrenoceptor antagoni...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199107000-00002
更新日期:1991-07-01 00:00:00
abstract::The dihydropyridine calcium antagonist nitrendipine offers a pathophysiologically based antihypertensive treatment with a potent dilation of resistance vessels, increased arterial compliance, and an acute natriuretic/diuretic response. Prolonged nitrendipine treatment in essential hypertension is not associated with s...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
doi:10.1097/00005344-198806124-00004
更新日期:1988-01-01 00:00:00
abstract::Cardiotrophin-1 (CT-1) a novel IL-6-related cytokine, induces distinct hypertrophic responses to endothelin-1 (ET-1) on cultured neonatal rat cardiac myocytes. We found that ET-1 and CT-1 show a distinct pattern of gene induction of natriuretic peptides. Elucidation of the transcriptional mechanisms of brain natriuret...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199800001-00099
更新日期:1998-01-01 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::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::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::Conflicting evidence has been reported on the hypothesis that vascular nitric oxide (NO) release is modulated by autonomic influences. Another controversial question is whether an insufficient degree of NO-dependent vasodilation may play a contributory role in the genesis of arterial hypertension. To address these que...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200111002-00006
更新日期:2001-11-01 00:00:00
abstract::We investigated mechanisms by which denopamine produces bell-shaped, cumulative concentration-response curves for positive inotropic effect in canine right ventricular muscle. As in our previous study, the curves ascended at 10(-8) to 10(-6) M, reached a maximum at 3 X 10(-6) to 10(-5) M, and descended at higher conce...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198910000-00008
更新日期:1989-10-01 00:00:00
abstract::The majority of deaths attributable to hypertension are coronary artery disease (CAD) deaths and, consequently, the prevention of CAD should be the primary aim of hypertension management. Recent meta-analyses confirm the results of the individual hypertension intervention trials, which demonstrated a disappointing sho...
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 short half-life, low plasma concentrations, and extensive biotransformation of prazosin suggest that it might be subject to extensive first-pass metabolism. Bioavailability, disposition, and hepatic extraction were studied in the dog. In conscious dogs whole blood prazosin concentrations were measured after oral a...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-197911000-00005
更新日期:1979-11-01 00:00:00
abstract::The degree of cardiac and vascular beta-adrenoceptor blockade of bisoprolol and atenolol was determined by the chronotropic dose 25 (CD25) of isoproterenol (the dose of an intravenous isoproterenol bolus required to increase resting heart rate by 25 beats/min) and by the increase in forearm blood flow (venous occlusio...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章
doi:10.1097/00005344-198511001-00010
更新日期:1986-01-01 00:00:00
abstract::In this study, we compared the effects of nitrendipine (20-40 mg daily) and enalapril (20-40 mg daily) in 44 patients with mild to moderate essential hypertension. After a 4-week placebo period, the patients entered a double-blind, crossover study of 16 weeks, divided by a second 4-week placebo period. Sitting and sta...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:1991-01-01 00:00:00
abstract::A significant reduction of maximal vasodilation capacity at the calf in relation to the severity of the hypertensive state has been demonstrated in essential hypertension. The aim of this study was to evaluate the behavior of calf blood flow and vascular resistance in borderline hypertensives (BH) in comparison with n...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198608005-00025
更新日期:1986-01-01 00:00:00
abstract::A double-blind randomised, parallel, placebo-controlled study was performed in patients with congestive heart failure, at 13 centres in 10 countries, to assess the efficacy and safety of lisinopril, a new angiotensin-converting enzyme inhibitor. After a 2-week run-in period, 130 patients receiving digoxin and/or diure...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00005344-198700003-00021
更新日期:1987-01-01 00:00:00
abstract::It is already well known that alteration of angiotensin II (Ang II) receptors results in cardiac remodeling in different pathological states, and it is believed that Ang II stimulates the release of endothelin-1 (ET-1). The present study aimed at investigating the interaction between ET-1 and different Ang II receptor...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000166223.57970.5f
更新日期:2004-11-01 00:00:00
abstract::Although evidence has been accumulated to support a role of endothelin-1 (ET-1) in cardiac hypertrophy, details of the pathophysiological significance of ET-1 in cardiac hypertrophy remain to be elucidated. In the present study, we investigated the effects of the vasodilator hydralazine on the blood pressure, cardiac ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-200036051-00054
更新日期:2000-11-01 00:00:00
abstract::Nicorandil, ATP sensitive potassium channel opener, is shown to reduce coronary events for patients with stable angina. The present study was designed to examine the protective potential of nicorandil for patients undergoing off-pump coronary artery bypass grafting. Twenty-four patients undergoing off-pump coronary ar...
journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:2004-10-01 00:00:00
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198205000-00004
更新日期:1982-05-01 00:00:00
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199602000-00007
更新日期:1996-02-01 00:00:00
abstract::The effects of bPTH-(1-34), a synthetic preparation of bovine parathyroid hormone containing the first 34 amino acids, on electromechanical activity of isolated rabbit sinus node cells and guinea pig papillary muscles were examined by microelectrode techniques. In sinus node cells, bPTH-(1-34) (10(-7) M) decreased the...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-198805000-00016
更新日期:1988-05-01 00:00:00
abstract::Cardiac endothelial nitric oxide synthase (ecNOS) was suppressed and inducible NOS (iNOS) enhanced at the decompensated heart failure stage in 18-week-old Dahl salt-sensitive (DS) hypertensive rats to which a high-salt diet had been administered from the age of 6 weeks. Nicorandil (NIC) enhanced ecNOS by activating Ad...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/01.fjc.0000211741.47960.c2
更新日期:2006-05-01 00:00:00
abstract::The preproendothelin-1 (preproET-1) gene is induced by thrombin after phosphorylation of nonreceptor protein tyrosine kinase pathways. This study investigated the contribution of Ca2+/calmodulin-dependent intracellular signaling cascades to this pathway and measured ET-1 mRNA levels by Northern blot analysis in human ...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1995-01-01 00:00:00
abstract::To clarify further the relationships between parathyroid glands and the development of hypertension, we studied the effect of cross-transplantation of these glands from young hypertensive rats in normotensive recipients. The parathyroid glands were isolated in 5-week-old hypertensive rats of the Lyon (male and female)...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:
更新日期:1994-01-01 00:00:00
abstract::A randomized open-label clinical trial was conducted to determine whether mortality, readmission, or quality of life differed between heart failure patients managed with captopril plus diuretics and those with digoxin plus diuretics. A total of 345 heart failure patients in New York Heart Association functional classe...
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:10.1097/00005344-199905000-00009
更新日期:1999-05-01 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
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更新日期:2020-10-01 00:00:00
abstract::We investigated the impact of respiratory syncytial virus (RSV) infection, an important asthma precipitant, on endothelin receptor function and release in sheep bronchial explants. RSV infection was confirmed using polymerase chain reaction and immunohistochemistry. Since sheep airway smooth muscle contains only endot...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
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更新日期:2004-11-01 00:00:00
abstract::The mechanism by which nicotine causes peripheral vasoconstriction and its relationship to the increased risk of peripheral vascular disease in smokers are unknown. To study the peripheral vascular effects of nicotine, we measured hemodynamic responses and oxygen consumption of the in situ gracilis muscle during intra...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/00005344-199110000-00009
更新日期:1991-10-01 00:00:00
abstract::Cardiac fibroblasts are the major non-myocyte cell constituent in the myocardium, and they are involved in heart remodeling. Angiotensin II type 1 receptor (AT1R) mediates the established actions of angiotensin II (Ang II), and changes in its expression have been reported in cardiac fibroblasts after myocardial infarc...
journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
doi:10.1097/FJC.0b013e318181fadd
更新日期:2008-08-01 00:00:00