Transient outward current inhibition by propafenone and 5-hydroxypropafenone in cultured neonatal rat ventricular myocytes.

Abstract:

:The antiarrhythmic agent propafenone and its primary electropharmacologically active metabolite, 5-hydroxypropafenone, are known inhibitors of cardiac myocyte repolarizing currents. We recently documented potent propafenone inhibition of the transient outward potassium current (Ito) in human atrial myocytes from patients in the newborn and infant age range. In the current study we characterized ventricular Ito inhibition by propafenone and 5-hydroxypropafenone in neonatal myocytes enzymatically isolated from 2-day-old Sprague-Dawley rat pups. Using the whole-cell patch-clamp technique in ventricular myocytes kept in primary culture for 1-4 days, we observed comparably potent Ito inhibition by both agents, yielding 50% maximal inhibitory concentration (IC50) values of 2.1 +/- 0.5 and 1.5 +/- 0.2 microM for propafenone and 5-hydroxypropafenone, respectively. Ito blockade by both of these agents was time, concentration, and voltage dependent, but use independent. There was no drug effect on steady-state voltage dependence of Ito inactivation, or on the time course of Ito recovery from inactivation. These findings are consistent with an open channel-blocking mechanism as suggested by other models. We conclude that both propafenone and 5-hydroxypropafenone are potent Ito inhibitors in neonatal rat ventricular myocytes, with potencies exceeding those demonstrated for propafenone in adult rat ventricular myocytes or in human atrial myocytes from patients of all ages.

journal_name

J Cardiovasc Pharmacol

authors

Cahill SA,Kirshenbaum LA,Gross GJ

doi

10.1097/00005344-200109000-00014

subject

Has Abstract

pub_date

2001-09-01 00:00:00

pages

460-7

issue

3

eissn

0160-2446

issn

1533-4023

journal_volume

38

pub_type

杂志文章
  • Metformin improves peripheral vascular flow in nonhyperlipidemic patients with arterial disease.

    abstract::The clinical activity of metformin (N,N-dimethyl biguanide), a widely used antidiabetic agent, on arterial blood flow was evaluated in 15 patients with peripheral atherosclerosis. Flow was determined by quantitative strain-gauge plethysmography; plasma lipid, lipoprotein, and apoprotein levels were repeatedly tested d...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-198409000-00027

    authors: Sirtori CR,Franceschini G,Gianfranceschi G,Sirtori M,Montanari G,Bosisio E,Mantero E,Bondioli A

    更新日期:1984-09-01 00:00:00

  • Comparison of angiotensin-converting enzyme inhibition with angiotensin II receptor antagonism in the human forearm.

    abstract::The object of this study was to differentiate losartan, an AT1-selective angiotensin II (ANG II) receptor antagonist, from enalapril, an angiotensin-converting enzyme (ACE) inhibitor, by measuring forearm vascular responses to AI, AII, and bradykinin. Eight healthy men were studied in a randomised, 4-period crossover ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-199310000-00011

    authors: Cockcroft JR,Sciberras DG,Goldberg MR,Ritter JM

    更新日期:1993-10-01 00:00:00

  • Effect of albumin on the electrophysiologic stability of isolated perfused rabbit hearts.

    abstract::The electrophysiologic stability of isolated perfused rabbit hearts was evaluated over a period of 5 h. Hearts perfused with protein-free buffer deteriorated over time, with significant shortening of the ventricular effective refractory period (ERP) and development of ventricular fibrillation. When serum albumin (6.01...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Kates RE,Yee YG,Hill I

    更新日期:1989-01-01 00:00:00

  • Negative inotropic effect of methylecgonidine, a major product of cocaine base pyrolysis, on ferret and human myocardium.

    abstract::This study examined the physiological effects and potential mechanisms of action of methylecgonidine (MEG), the major pyrolysis product from smoking "crack cocaine," on cardiac function. Ferret right ventricular papillary muscles and human ventricular trabeculae were isolated and placed in a physiological solution at ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199709000-00013

    authors: Woolf JH,Huang L,Ishiguro Y,Morgan JP

    更新日期:1997-09-01 00:00:00

  • Efficacy of ajmaline and propafenone in patients with accessory pathways: a prospective randomized study.

    abstract::In a prospective randomized study, we assessed the electrophysiologic effects and the efficacy of ajmaline versus propafenone in patients with accessory pathways (APs). During initiated atrioventricular (AV) reentrant tachycardia or atrial fibrillation (AF), ajmaline (1 mg/kg as bolus followed by infusion of 15 microg...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-199410000-00018

    authors: Chen X,Borggrefe M,Martinez-Rubio A,Hief C,Haverkamp W,Hindricks G,Breithardt G

    更新日期:1994-10-01 00:00:00

  • Treatment of heart failure: state of the art and prospectives.

    abstract::Heart failure is unique among the major cardiovascular disorders in that it alone is increasing in prevalence while there has been a striking decrease in other conditions. Some of this can be attributed to the aging of the U.S. and European populations. The ability to salvage patients with myocardial damage is also a ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-200111002-00015

    authors: Greenberg B

    更新日期:2001-11-01 00:00:00

  • Neuropeptide-Y-ATP interactions at the vascular sympathetic neuroeffector junction.

    abstract::Neuropeptide Y (NPY) and ATP are considered cotransmitters with norepinephrine (NE) in sympathetic neurons innervating some blood vessels, including those of the mesentery. A prominent action of NPY is to potentiate the postjunctional contractile effect of NE as well as that of other vasoactive agents. We wished to in...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199511000-00002

    authors: Westfall TC,Yang CL,Curfman-Falvey M

    更新日期:1995-11-01 00:00:00

  • Amlodipine inhibition of serum-, thrombin-, or fibroblast growth factor-induced vascular smooth-muscle cell proliferation.

    abstract::Atherosclerosis, like several other vascular diseases, exhibits structural and functional abnormalities resulting partially from an exaggerated proliferation of vascular smooth-muscle cells (VSMCs). Ca2+ channel blockers, such as amlodipine, have been suggested to retard or even prevent the progression of atherosclero...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199805000-00019

    authors: Stepien O,Gogusev J,Zhu DL,Iouzalen L,Herembert T,Drueke TB,Marche P

    更新日期:1998-05-01 00:00:00

  • Bremazocine causes sympatho-inhibition and hypotension in rabbits by activating peripheral kappa-receptors.

    abstract::We have studied the effects of bremazocine on the peripheral sympathetic nervous system and the arterial blood pressure of pithed rabbits with electrically (2 Hz) stimulated sympathetic outflow, and compared them with the effects of Leu-enkephalin and fentanyl. The 3H-noradrenaline plasma clearance and the plasma conc...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198605000-00005

    authors: Ensinger H,Hedler L,Szabo B,Starke K

    更新日期:1986-05-01 00:00:00

  • Effect of different calcium channel blockers on angiotensin II- and vasopressin-induced prostacyclin biosynthesis in vascular smooth muscle cells.

    abstract::To gain insight with regard to the mode of action of calcium antagonists on the vasculature, we examined the effects of nifedipine, isradipine, felodipine, verapamil, gallopamil, and amlodipine on vasoconstrictor-induced prostacyclin synthesis in vitro. Cultured rat aortic smooth muscle cells were seeded after two to ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199004000-00012

    authors: Vallotton MB,Gerber-Wicht C,Dolci W,Rivest RW

    更新日期:1990-04-01 00:00:00

  • Effects of tocainide enantiomers on experimental arrhythmias produced by programmed electrical stimulation.

    abstract::The enantiomers of tocainide, a Class Ib antiarrhythmic agent, have recently been shown to exhibit differences in antiarrhythmic activity and pharmacokinetic characteristics. The present study examined the antiarrhythmic and electrophysiological effects of SR tocainide, S tocainide, and R tocainide on arrhythmias in a...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Uprichard AC,Allen JD,Harron DW

    更新日期:1988-02-01 00:00:00

  • Effect of bopindolol on renin secretion and renal excretory function in rats.

    abstract::We investigated the effects of the new beta-adrenoceptor antagonist, bopindolol, on stimulated renin secretion and on renal function in conscious rats. Intravenous doses of 10, 31.6, and 100 micrograms/kg of bopindolol antagonized the rise in plasma renin activity (PRA) induced by the administration of isoproterenol (...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198906000-00008

    authors: Proakis AG,Barrett RJ,Anderson LA,Wright KF,Taylor DR

    更新日期:1989-06-01 00:00:00

  • Alpha 2-adrenoceptor agonists in the treatment of hypertension.

    abstract::Alpha 2-adrenoceptor agonists are effective antihypertensive drugs that may provide particular advantages in the treatment of many types of patients. Of those now available, guanabenz has been shown to lower serum cholesterol concentration and not to cause sodium and water retention, offering additional protection aga...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Kaplan NM

    更新日期:1985-01-01 00:00:00

  • Augmented response of endothelin-A and endothelin-B receptor stimulation in coronary arteries of hypertensive hearts.

    abstract::To determine whether the vasoconstrictor response to endothelin-1 (ET-1) is altered in coronary vessels of hypertensive hearts and the role of ETA and ETB receptors in these responses to ET-1, the vasoconstrictor response to ET-1 in coronary vessels was measured with or without ETA and ETB receptor antagonists. In iso...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199800001-00029

    authors: Miki S,Takeda K,Kiyama M,Hatta T,Morimoto S,Kawa T,Itoh H,Nakata T,Sasaki S,Nakagawa M

    更新日期:1998-01-01 00:00:00

  • Time course of spirapril-induced structural and functional changes after myocardial infarction in rats followed with magnetic resonance imaging.

    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

    authors: Zierhut W,Rudin M,Robertson E,Zerwes HG,Novosel D,Evenou JP,Stirnimann R,Hof RP

    更新日期:1993-06-01 00:00:00

  • Influence of endogenous neuropeptide Y (NPY) on the sympathetic-parasympathetic interaction in the canine heart.

    abstract::The purpose of this study was to examine the sympathetic-parasympathetic interactions on heart rate through release of neuropeptide Y (NPY) and its action on prejunctional NPY Y2 receptors on vagal and sympathetic nerve fibers. In other studies on various preparations and in various organs, attenuation of transmitter ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/01.fjc.0000177986.21929.d8

    authors: Ilebekk A,Björkman JA,Nordlander M

    更新日期:2005-10-01 00:00:00

  • Effectiveness and Safety of Bivalirudin During Percutaneous Coronary Intervention in Acute Coronary Syndrome in the Real World: CARTAGOMAX Study.

    abstract::The CARTAGOMAX study assessed the safety and efficacy of bivalirudin during real-world cardiac intervention. This was a single-center prospective study. Patients with acute coronary syndrome undergoing percutaneous coronary intervention were anticoagulated with bivalirudin alone or unfractionated heparin plus a glycop...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/FJC.0000000000000411

    authors: Cascón-Pérez JD,Abellán-Huerta J,Giner-Caro JA,Dau-Villareal DF,Mármol-Lozano R,Jaulent-Huertas L,Bonilla-Pacheco YI,Ruiz-Abellón Mdel C,Picó-Aracil F,Castillo-Moreno JA

    更新日期:2016-09-01 00:00:00

  • Hemodynamic effects of isoprostanes (8-iso-prostaglandin F2alpha and E2) in isolated guinea pig hearts.

    abstract::Isoprostanes are a family of prostaglandin-related compounds formed from arachidonic acid in a cyclooxygenase-independent manner as products of free radical-initiated lipid peroxidation. To elucidate the biological activity of the F2-and E2-isoprostanes, 8-iso-prostaglandin F2alpha (8-iso-PGF2alpha) and 8-iso-prostagl...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-199706000-00012

    authors: Möbert J,Becker BF,Zahler S,Gerlach E

    更新日期:1997-06-01 00:00:00

  • Vascular smooth muscle energetics.

    abstract::ATP utilization (delta approximately P) during an isometric contraction has been studied in terms of both measurements of oxygen consumption and lactate production as well as of the tissue nucleotide and metabolite levels. The contribution of breakdown of preformed ATP and phosphocreatine (PCr) pools to delta approxim...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1097/00005344-198406002-00006

    authors: Paul RJ,Krisanda JM,Lynch RM

    更新日期:1984-01-01 00:00:00

  • Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats.

    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

    authors: Traupe T,Ortmann J,Haas E,Münter K,Parekh N,Hofmann-Lehmann R,Baumann K,Barton M

    更新日期:2006-03-01 00:00:00

  • Renal function, body fluid volumes, renin, aldosterone, and noradrenaline during treatment of hypertension with pindolol.

    abstract::Sixteen hypertensive patients received pindolol (10-45 mg/day); mean +/- SD, 28.75 +/- 15.22) for 3-8 weeks in a placebo-controlled, single-blind, crossover study. Supine and standing blood pressures (BP) were lowered, whereas effective renal plasma flow and glomerular filtration rates (estimated from the clearances o...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00005344-198105000-00018

    authors: Wilcox CS,Lewis PS,Peart WS,Sever PS,Osikowska BA,Suddle SA,Bluhm MM,Veall N,Lancaster R

    更新日期:1981-05-01 00:00:00

  • Effect of acute and chronic indoramin administration on baroreflex function and tremor in humans.

    abstract::Several mechanisms have been suggested for the absence of reflex tachycardia in response to the hypotensive effect of the selective alpha 1-adrenoceptor antagonist indoramin, including, in animals, membrane-stabilising activity, prolongation of repolarisation time, and reduction in baroreflex sensitivity. The present ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1097/00005344-198803000-00004

    authors: Deering AH,Riddell JG,Harron DW,Shanks RG

    更新日期:1988-03-01 00:00:00

  • Bisoprolol improves survival in rats with heart failure.

    abstract::The cardioprotective effects of bisoprolol were studied in a rat model of severe heart failure induced by autoimmune myocarditis. Twenty-eight days after immunization, Lewis rats were divided into four groups: 0.1 mg/kg/day bisoprolol (Group 0.1), 1.0 mg/kg/day bisoprolol (Group 1) and 10 mg/kg/day bisoprolol (Group 1...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-200110001-00012

    authors: Watanabe K,Ohta Y,Inoue M,Ma M,Wahed MI,Nakazawa M,Hasegawa G,Naito M,Fuse K,Ito M,Kato K,Hanawa H,Kodama M,Aizawa Y

    更新日期:2001-10-01 00:00:00

  • Activation of IK1 channel by zacopride attenuates left ventricular remodeling in rats with myocardial infarction.

    abstract::Activating IK1 channels is considered to be a promising antiarrhythmic strategy. Zacopride has been identified as a selective IK1 channel agonist and can suppress triggered arrhythmias. Whether this drug also exerts a beneficial effect on cardiac remodeling is unknown, and the present study sought to address this ques...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章,收录出版

    doi:10.1097/FJC.0000000000000127

    authors: Liu CF,Liu QH,Liu EL,Zhai XW,Zhang L,Luo TE,Zhang WF,Feng QL,Cui XL,Zhao ZQ,Cao JM,Wu BW

    更新日期:2014-10-01 00:00:00

  • Prostacyclin does not inhibit rho-kinase: an implication for the treatment of pulmonary hypertension.

    abstract::Primary pulmonary hypertension continues to be a fatal disease. We have recently demonstrated that long-term inhibition of Rho-kinase, an effector of the small GTPase Rho, is effective for the treatment of pulmonary hypertension (PH) in rats and humans. Prostacyclin has been clinically used for the treatment of PH wit...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/01.fjc.0000151898.65260.6a

    authors: Abe K,Morikawa K,Hizume T,Uwatoku T,Oi K,Seto M,Ikegaki I,Asano T,Kaibuchi K,Shimokawa H

    更新日期:2005-02-01 00:00:00

  • Synthesis and renin inhibitory properties of a new soluble pepstatin derivative.

    abstract::A new pepstatin derivative, pepstatinyl arginine methyl ester hydrochloride (pepstatinyl-Arg-O-Me), was synthesized with the aim of increasing water solubility without altering capacity to inhibit the renin-angiotensinogen reaction. Pepstatinyl-Arg-O-Me was shown to inhibit in vitro the reaction between either rat or ...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198009000-00017

    authors: Gardes J,Evin G,Castro B,Corvol P,Menard J

    更新日期:1980-09-01 00:00:00

  • Reduction of aldosterone production improves renal oxidative stress and fibrosis in diabetic rats.

    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

    authors: Matavelli LC,Siragy HM

    更新日期:2013-01-01 00:00:00

  • International cooperative study on the relationship between dietary factors and blood pressure: a report from the Cardiovascular Diseases and Alimentary Comparison (CARDIAC) Study.

    abstract::To investigate the epidemiological relationship of dietary factors to blood pressure (BP) and major cardiovascular diseases, we carried out the International Cooperative Cardiovascular Diseases and Alimentary Comparison (CARDIAC) Study, which so far involves 45 centers in 20 countries. From each population, 100 men an...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:

    authors: Yamori Y,Nara Y,Mizushima S,Mano M,Sawamura M,Kihara M,Horie R

    更新日期:1990-01-01 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

  • Effects of verapamil on accessory pathway properties and induction of circus movement tachycardia in patients with the Wolf-Parkinson-White syndrome.

    abstract::The electrophysiological effects of 0.2 mg/kg of intravenously administered verapamil (mean plasma level, 51.3 ng/ml) were evaluated using intracardiac recordings and electrical stimulation in 10 patients with the concealed or manifest Wolff-Parkinson-White syndrome. Verapamil produced a minimal effect on both the ant...

    journal_title:Journal of cardiovascular pharmacology

    pub_type: 杂志文章

    doi:10.1097/00005344-198101000-00002

    authors: Matsuyama E,Konishi T,Okazaki H,Matsuda H,Kawai C

    更新日期:1981-01-01 00:00:00