Oral naftidrofuryl prevents platelet hyperreactivity ex vivo and inhibits functional desensitization to prostacyclin in hypercholesterolemic rabbits.

Abstract:

:Among other mediators, platelet-derived serotonin (5-HT) may contribute to thromboembolic complications of atherosclerosis. We determined whether long-term oral treatment with the 5-HT2 antagonist naftidrofuryl (NAF, 50 mg/kg daily for 12 weeks) alters platelet function in cholesterol-fed (1%) rabbits. Hypercholesterolemia resulted in marked platelet hyperreactivity to collagen and ADP. This included increased aggregation, ATP secretion, and thromboxane formation; e.g., collagen-induced (1.2 micrograms/ml) platelet aggregation was stimulated to 210 +/- 10 mm/30 s in cholesterol-fed rabbits as compared with 108 +/- 9 mm/30 s in rabbits fed a standard diet (p < 0.05). Inhibition of ADP-stimulated platelet activation by the prostacyclin mimetic iloprost was significantly reduced. NAF did not reduce plasma cholesterol in hypercholesterolemia, but prevented enhanced platelet aggregation, thromboxane formation, and ATP secretion. NAF treatment significantly reduced collagen-induced (1.2 micrograms/ml) aggregation to 81 +/- 20 mm/30 s in these animals (p < 0.05). NAF also inhibited functional desensitization of platelets to iloprost, but did not alter the impaired binding of [3H]iloprost to platelet membranes in hypercholesterolemic animals. NAF also did not change any of these parameters in normocholesterolemic rabbits. These data suggest beneficial effects of NAF on platelet hyperreactivity in experimental hypercholesterolemia which may also be relevant for its clinical use.

journal_name

J Cardiovasc Pharmacol

authors

Weber AA,Hohlfeld T,Strobach H,Schrör K

doi

10.1097/00005344-199302000-00021

subject

Has Abstract

pub_date

1993-02-01 00:00:00

pages

332-8

issue

2

eissn

0160-2446

issn

1533-4023

journal_volume

21

pub_type

杂志文章
  • Evidence for presynaptic inhibitory histamine (H2) receptors in the rat hindquarter vasculature.

    abstract::Histamine released within walls of resistance blood vessels is suggested to mediate an active portion of baroreceptor-mediated neurogenic vasodilatation in skeletal muscle vasculature. Studies were undertaken to examine the possibility that histamine-mediated active vasodilatation could be effected, in part, by an inh...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198706000-00003

    authors: Holcslaw TL,Lassiter D

    更新日期:1987-06-01 00:00:00

  • Growth control and morphogenesis in the development and pathology of arteries.

    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

    authors: Schwartz SM,Liaw L

    更新日期:1993-01-01 00:00:00

  • Potentiating effects on contractions by purified baicalin and baicalein in the rat mesenteric artery.

    abstract::The effects of purified baicalin and baicalein from the traditional Chinese herb, Huangqin, on contractions induced by phenylephrine, U46619, and high extracellular K+ were investigated in isolated rat mesenteric arteries. Both baicalin (1-100 microM) and baicalein (1-50 microM) potentiated the contractile response to...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-200008000-00018

    authors: Tsang SY,Chen ZY,Yao XQ,Huang Y

    更新日期:2000-08-01 00:00:00

  • Diltiazem inhibits the late increase in extracellular potassium by maintaining glycolytic ATP synthesis during myocardial ischemia.

    abstract::During myocardial ischemia, the extracellular potassium concentration increases in a triphasic pattern, an initial early increase, a constant phase, and a late increasing phase. The aim of this study was to determine whether diltiazem inhibits the late increasing phase by maintaining glycolytic adenosine triphosphate ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199710000-00004

    authors: Sakamoto K,Yamazaki J,Nagao T

    更新日期:1997-10-01 00:00:00

  • Effect of clentiazem (TA-3090) with posttreatment on neurologic and histologic disorders of stroke-prone spontaneously hypertensive rats with history of stroke.

    abstract::After stroke-prone spontaneously hypertensive rats (SHRSP) received a salt-loaded diet to accelerate onset of stroke, the therapeutic effect of clentiazem, a benzothiazepine Ca antagonist, on neurologic and histologic disorders was examined. Treatment with clentiazem (3, 15, and 30 mg/kg) orally twice daily (b.i.d.) f...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199401000-00023

    authors: Kikkawa K,Murata S,Kurosawa H,Toriumi W,Iwasaki H,Nagao T

    更新日期:1994-01-01 00:00:00

  • Peripheral alpha 2 adrenoceptor stimulation contributes to the sympatholytic effect of guanfacine in humans.

    abstract::Guanfacine 3 mg was infused into six volunteers over 1 h on two occasions to investigate whether its sympatholytic effect is centrally or peripherally mediated. On one occasion, the central effects of guanfacine were blocked by prior administration of idazoxan 0.2 mg/kg i.v. (45 min preguanfacine); central alpha 2-blo...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-198500076-00027

    authors: Brown MJ,Struthers AD,di Silvio L

    更新日期:1985-01-01 00:00:00

  • Sustained-release diltiazem and prevention of cardiovascular risk in hypertensive patients.

    abstract::The prevention of coronary disease in hypertensive patients will see progress in the years to come. It is clearly too much, however, to expect this progress to come exclusively from the application of new therapies, as the incidence of coronary disease in hypertensive patients depends on several factors, which are, es...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:

    authors: Djian J

    更新日期:1990-01-01 00:00:00

  • Toll-like receptor 4 inhibitor TAK-242 treatment does not influence perfusion recovery in tissue ischemia.

    abstract::Toll-like receptors (TLRs) are important in innate immune responses, which are crucial in collateral artery formation (arteriogenesis). TLR4⁻/⁻ mice undergoing hind limb ischemia show decreased perfusion recovery accompanied by an impaired infiltration of inflammatory cells. TLR antagonists are currently developed and...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0000000000000019

    authors: van den Borne P,Bastiaansen AJ,de Vries MR,Quax PH,Hoefer IE,Pasterkamp G

    更新日期:2014-01-01 00:00:00

  • Effects of antihypertensive drugs on atherogenic factors: possible importance of drug selection in prevention of atherosclerosis.

    abstract::The treatment of hypertension is clearly beneficial. Blood pressure reduction with antihypertensive drugs reduces mortality and the incidence of complications such as stroke, renal failure, and congestive failure. However, analysis of long-term studies using different antihypertensive drugs indicates that the outcome ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Spence JD

    更新日期:1985-01-01 00:00:00

  • Efficacy of carvedilol in exercise-induced myocardial ischemia.

    abstract::The exercise response to a single oral dose (25 mg) of a new beta-blocking agent that also has potent vasodilating properties, carvedilol, was assessed in 15 patients with stable exertional angina, positive exercise tests (greater than or equal to 1 mm ST depression) and coronary artery disease. A placebo-controlled, ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Kaski JC,Rodriguez-Plaza L,Brown J,Maseri A

    更新日期:1987-01-01 00:00:00

  • Pharmacologic, metabolic, and toxicologic profile of spirapril (SCH 33844), a new angiotensin converting inhibitor.

    abstract::Spirapril (SCH 33844; 7-N-[1(S)-ethoxycarbonyl-3-phenylpropyl]-(S)-alanyl-1,4-dithia- 7-azaspiro[4,4]-nonane-8(S)-carboxylic acid) is a new angiotensin-converting enzyme (ACE) inhibitor. SCH 33844 diacid inhibited hydrolysis of hip-his-leu by rabbit lung ACE in a potent (Ki = 0.74 nM), selective, and noncompetitive fa...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198706107-00020

    authors: Sybertz EJ,Watkins RW,Ahn HS,Baum T,La Rocca P,Patrick J,Leitz F

    更新日期:1987-01-01 00:00:00

  • Antiarrhythmic and electrophysiologic effects of ibutilide in a chronic canine model of atrial flutter.

    abstract::We studied the effects of orally administered ibutilide, a class III antiarrhythmic agent, in a model of reentrant atrial flutter in conscious dogs. After baseline determination of atrial effective refractory period (AERP) and demonstration of reproducible induction of atrial flutter by rapid atrial pacing, 8 dogs rec...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199307000-00002

    authors: Buchanan LV,Turcotte UM,Kabell GG,Gibson JK

    更新日期:1993-07-01 00:00:00

  • Phase 1B, Randomized, Double-Blinded, Dose Escalation, Single-Center, Repeat Dose Safety and Pharmacodynamics Study of the Oral NLRP3 Inhibitor Dapansutrile in Subjects With NYHA II-III Systolic Heart Failure.

    abstract:ABSTRACT:The NLRP3 inflammasome has been implicated in the development and progression of heart failure. The aim of this study was to determine the safety of an oral inhibitor of the NLRP3 inflammasome, dapansutrile (OLT1177), in patients with heart failure and reduced ejection fraction (HFrEF). This was a phase 1B, ra...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0000000000000931

    authors: Wohlford GF,Van Tassell BW,Billingsley HE,Kadariya D,Canada JM,Carbone S,Mihalick VL,Bonaventura A,Vecchié A,Chiabrando JG,Bressi E,Thomas G,Ho AC,Marawan AA,Dell M,Trankle CR,Turlington J,Markley R,Abbate A

    更新日期:2020-10-24 00:00:00

  • Slow channel inhibitors verapamil and nifedipine in the management of hypertension.

    abstract::The "Oxford" system for continuous monitoring of the ambulatory blood pressure was used to assess the changes in blood pressure following therapy with the calcium ion antagonists verapamil and nifedipine in two separate groups of patients. In the first group 16 patients were studied on both no therapy and following a ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Gould BA,Hornung RS,Mann S,Balasubramanian V,Raftery EB

    更新日期:1982-01-01 00:00:00

  • Impaired L-arginine uptake but not arginase contributes to endothelial dysfunction in rats with chronic kidney disease.

    abstract::Reduced nitric oxide bioavailability contributes to increased cardiovascular disease risk in patients with chronic kidney disease (CKD). Arginase has been implicated as a potential therapeutic target to treat vascular dysfunction by improving substrate availability for endothelial nitric oxide synthase. The purpose of...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0000000000000022

    authors: Martens CR,Kuczmarski JM,Lennon-Edwards S,Edwards DG

    更新日期:2014-01-01 00:00:00

  • Predominant alpha 1-adrenoceptor-mediated contraction in the human internal mammary artery.

    abstract::alpha-Adrenoceptor agonists and antagonists are widely used perioperatively for internal mammary artery (IMA)-coronary artery bypass operations. To determine subtypes of alpha-adrenoceptors in the human IMA, we studied responses of isolated human IMA segments to alpha-adrenoceptor agonists, antagonists, and electrical...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: He GW,Shaw J,Hughes CF,Yang CQ,Thomson DS,McCaughan B,Hendle PN,Baird DK

    更新日期:1993-02-01 00:00:00

  • Serotonin-induced vasoconstriction in the perfused canine femoral artery can be blocked in vivo by ketanserin.

    abstract::Serotonin, applied to helical strips of larger vessels such as coronary arteries, acts as a potent vasoconstrictor in vitro. In contrast, in vivo serotonin causes a remarkable decrease in total peripheral resistance. To differentiate the influence of serotonin on resistances of large and small vessels, experiments wer...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198500077-00017

    authors: Meschig R,Breuer J,Arnold G

    更新日期:1985-01-01 00:00:00

  • Resveratrol inhibits rat aortic vascular smooth muscle cell proliferation via estrogen receptor dependent nitric oxide production.

    abstract::Vascular smooth muscle cell (VSMC) proliferation is pivotal in the progression of hypertension, atherosclerosis, and restenosis. Resveratrol is a grape polyphenol that is implicated as an important contributor to red wine's vascular protective effects. Its antimitogenic action on VSMC is attributed to an array of plei...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0b013e318059ae80

    authors: Ekshyyan VP,Hebert VY,Khandelwal A,Dugas TR

    更新日期:2007-07-01 00:00:00

  • Vascular smooth muscle: availability of calcium through alpha-adrenoceptor stimulation.

    abstract::In strip preparations from the rabbit main pulmonary artery, it was not possible to differentiate convincingly between alpha 1- and alpha 2-adrenoceptors, when selective agonists such as methoxamine, St 587, B-HT 920, and clonidine, as well as selective antagonists such as prazosin and yohimbine were used for receptor...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Haeusler G,de Peyer JE,Yajima M,Schultz G

    更新日期:1986-01-01 00:00:00

  • Trimetazidine inhibits neutrophil accumulation after myocardial ischaemia and reperfusion in rabbits.

    abstract::Interventions that inhibit neutrophil infiltration into myocardial tissue after ischaemia and reperfusion are reported to reduce the size of the infarct. We examined whether administration of trimetazidine, which is reported to reduce myocardial infarct size, affects this process. [111In]Neutrophils and [125I]albumin ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199312000-00008

    authors: Williams FM,Tanda K,Kus M,Williams TJ

    更新日期:1993-12-01 00:00:00

  • Effect of nifedipine on cyclic GMP turnover in cultured coronary smooth muscle cells.

    abstract::We investigated the effects of nifedipine on cyclic GMP turnover and the pertinent enzyme activities in cultured coronary smooth muscle cells (SMC). Nifedipine at high concentrations slightly decreased basal soluble guanylate cyclase activity and inhibited the action of sodium nitroprusside (SNP) but had no effect on ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199510000-00013

    authors: Kishi Y,Watanabe T,Makita T,Sakita S,Watanabe R,Ashikaga T,Numano F

    更新日期:1995-10-01 00:00:00

  • Cardiovascular morbidity and mortality in HDFP patients 50-69 years old at entry.

    abstract::Five-year morbidity and mortality in the Hypertension Detection and Follow-Up Program (HDFP) were stratified by age groups at entry to the study and by Stepped Care (SC) and Referred Care (RC) treatment groups. Although the incidence of stroke increased with age in both treatment groups, the greatest reduction in stro...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198507002-00002

    authors: Maxwell MH,Ford CE

    更新日期:1985-01-01 00:00:00

  • Long-term effects of carvedilol on left ventricular function, remodeling, and expression of cardiac cytokines after large myocardial infarction in the rat.

    abstract::Carvedilol (20 mg/kg, bid) or vehicle was given to rats surviving a myocardial infarction (MI) 24 h (n = 409). In rats with large MI, carvedilol partially preserved left ventricular (LV) function and intrinsic myocardial contractility and reactivity to beta-adrenergic stimulation. Carvedilol led to scar thickening, in...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-200201000-00009

    authors: Sia YT,Parker TG,Tsoporis JN,Liu P,Adam A,Rouleau JL

    更新日期:2002-01-01 00:00:00

  • Effects of temocapril and olmesartan on myocardial sympathetic nervous activity and fatty acid metabolism in rats with chronic beta-adrenergic stimulation.

    abstract::We investigated the effects of an angiotensin-converting enzyme inhibitor (temocapril) and an angiotensin II type 1 receptor blocker (olmesartan) on changes in myocardial sympathetic nervous activity, fatty acid metabolism and myocardial blood flow using 131I-meta-iodobenzylguanidine, 125I-beta-methyl-iodophenyl penta...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Ido A,Hasebe N,Takeuchi T,Kikuchi K

    更新日期:2003-01-01 00:00:00

  • Pharmacokinetic-pharmacodynamic relations of losartan and EXP3174 in a porcine animal model.

    abstract::The pharmacokinetics of losartan and EXP3174, an active metabolite of losartan, were evaluated in the anesthetized pig after both a single intravenous dose (3 mg/kg) and during constant intravenous infusion. The pharmacodynamic activities of losartan and EXP3174 were determined during constant intravenous infusion as ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199711000-00008

    authors: Lankford SM,Plummer D,Hellyer P,Christ DD,Bai SA

    更新日期:1997-11-01 00:00:00

  • Pharmacokinetics of amiodarone in man.

    abstract::We studied the kinetics of amiodarone in three healthy volunteers after single oral (400 mg) and intravenous (150 mg) doses and in six patients with supraventricular tachycardia. Three patients were studied after the first oral dose (400 mg) and during subsequent therapy (200 mg/day); the other three after 5 mg/kg of ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198203000-00015

    authors: Riva E,Gerna M,Latini R,Giani P,Volpi A,Maggioni A

    更新日期:1982-03-01 00:00:00

  • Comparative effects of antihypertensive therapy with guanabenz and propranolol on renal vascular resistance and left ventricular mass.

    abstract::There is increasing interest in initial therapy of hypertension with sympatholytic agents and the influence of antihypertensive therapy on cardiac and renal function. We treated 26 men with essential hypertension with either guanabenz alone (n = 14) or propranolol alone (n = 12) and assessed blood pressure and renal p...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Mosley C,O'Connor DT,Taylor A,Slutsky RA,Cervenka J

    更新日期:1984-01-01 00:00:00

  • New method of investigating functional roles of pressure-sensitive mechanoreceptor in human endothelial cells.

    abstract::The role of pressure-sensitive mechanoreceptors (PSMRs) in histamine-stimulated nitric oxide release from cultured human endothelial cells was investigated, using our new method (helium pack method). PSMRs were stimulated by various levels of pressure applied in addition to atmospheric pressure (40, 80, 120, and 160 m...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199204002-00020

    authors: Hishikawa K,Nakaki T,Suzuki H,Saruta T,Kato R

    更新日期:1992-01-01 00:00:00

  • The pathway-selective estrogen receptor ligand WAY-169916 displays differential activity in ischemia-reperfusion injury models.

    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

    authors: Harnish DC,Liu X,Kenney T,Winneker RC,Chadwick C,Friedrichs GS,Kilbourne EJ

    更新日期:2006-06-01 00:00:00

  • Hemodynamic response to adenosine infusion before and after coronary artery bypass surgery.

    abstract::This study describes the hemodynamic dose-response characteristics of a titrated, continuous adenosine infusion before and 1 h (anesthetized), 1 week, and 1 year after coronary artery bypass graft (CABG) surgery. Average tolerated adenosine infusion rates were less 1 h and 1 week after surgery (128 +/- 23 and 118 +/- ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199703000-00005

    authors: Anderson RE,Lind B,Owall A,Brodin LA

    更新日期:1997-03-01 00:00:00