Electrophysiological effects of E‐3753, a new antiarrhythmic drug, in guinea‐pig ventricular muscle

@article{Delpn1989ElectrophysiologicalEO,
  title={Electrophysiological effects of E‐3753, a new antiarrhythmic drug, in guinea‐pig ventricular muscle},
  author={Eva Delp{\'o}n and Carmen Valenzuela and Juan Tamargo},
  journal={British Journal of Pharmacology},
  year={1989},
  volume={96}
}
1 The electrophysiological effects of E‐3753, a new antiarrhythmic drug, were studied in guinea‐pig papillary muscles. 2 E‐3753 (10−7‐10−4m) produced a concentration‐dependent decrease in the action potential amplitude and Vmax of the upstroke, shortened the action potential duration (APD) and shifted the resting membrane potential to less negative values. E‐3753 also shortened the effective refractory period (ERP), lengthening the ERP relative to APD. 3 E‐3753 (10−5m) shifted the membrane… 
11 Citations
Electrophysiological effects of CRE‐1087 in guinea‐pig ventricular muscles
TLDR
The slow onset and the slow offset kinetics of frequency‐dependent Vmax block during repetitive activity suggested that in guinea‐pig ventricular muscle fibres CRE‐1087 exhibited class Ic antiarrhythmic actions.
Electrophysiological effects of CI‐980, a tubulin binding agent, on guinea‐pig papillary muscles
TLDR
It is concluded that in guinea‐pig papillary muscles, CI‐980 produces a use‐dependent inhibition of Vmax and a reverse use‐ dependent prolongation of the ventricular action potential, thus exhibiting class I and class III antiarrhythmic actions, respectively.
Electrophysiological e ects of CI-980 , a tubulin binding agent , on guinea-pig papillary muscles
TLDR
It is concluded that in guinea-pig papillary muscles, CI-980 produces a use-dependent inhibition of Vmax and a reverse use- dependent prolongation of the ventricular action potential, thus exhibiting class I and class III antiarrhythmic actions, respectively.
Effects of lisinopril on electromechanical properties and membrane currents in guinea‐pig cardiac preparations
TLDR
The results indicate that the negative inotropic effect of lisinopril cannot be explained by a decrease in Ca2+ entry through L‐type channels and suggest that lisinobril may possibly act at an intracellular site to reduce contractile force.
Effects of the two enantiomers, S‐16257‐2 and S‐16260‐2, of a new bradycardic agent on guinea‐pig isolated cardiac preparations
TLDR
It can be concluded that S57 and R60, the two enantiomers of the new bradycardic agent, produced a similar frequency‐dependent Vmax block which indicated that the interaction with the Na+ channel was not stereospecific.
Electrophysiological effects of the combination of mexiletine and flecainide in guinea‐pig ventricular fibres
TLDR
It is concluded that the combination of mexiletine and flecainide is synergistic at driving rates faster than 0.5 Hz without detracting from the characteristics of flecains, and was more effective in inhibiting the Vmax of early test stimuli than either drug alone.
Effects of platelet activating factor on contractile force and 45Ca fluxes in guinea‐pig isolated atria
TLDR
The results suggest that in guinea‐pig atria the biphasic inotropic effects of PAF cannot be explained through modifications in the slow inward Ca2+ current or in Na+‐Ca2+ exchange, but may be related to changes in trans‐sarcolemmal Ca 2+ entry mediated by specific PAF receptors.
Antiarrhythmic drug research
  • M. Walker
  • Biology
    British journal of pharmacology
  • 2006
TLDR
This article discusses antiarrhythmic drug research conducted by members of BPS, and as published in the British Journal of Pharmacology, but only quotes selected manuscripts and individuals.
...
...

References

SHOWING 1-10 OF 35 REFERENCES
Tonic and Phasic Vmax Block Induced by 5‐Hydroxypropafenone in Guinea Pig Ventricular Muscles
TLDR
Findings suggest that 5-OH-P exhibited similar phasic inhibitory action of the fast sodium channels than other class Ic antiarrhythmic drugs.
VOLTAGE‐ AND TIME‐DEPENDENT DEPRESSION OF MAXIMUM RATE OF DEPOLARIZATION OF GUINEA‐PIG VENTRICULAR ACTION POTENTIALS BY TWO STEROIDAL ANTIARRHYTHMIC DRUGS, CCI 22277 AND ORG 6001
TLDR
Both steroidal anti‐arrhythmic drugs shifted the steady‐state inactivation curve, relating V̇max to resting membrane potential, in the hyperpolarizing direction, implying selective depression of depolarized cells.
Electrophysiological Effects of 5‐Hydroxypropafenone on Guinea Pig Ventricular Muscle Fibres
TLDR
5-OH-P is an active metabolite which exhibits class 1 antiarrhythmic effects and which may be responsible for some of the cardiodepressant and antiarrythmic effects previously described for propafenone.
Test of a Model of Antiarrhythmic Drug Action Effects of Quinidine and Lidocaine on Myocardial Conduction
TLDR
The effects of quinidine and lidocaine on the maximum upstroke velocity of the ventricular myocardial action potential were compared with the effects predicted by a model over a wide range of driving rates, rhythm disturbances and holding potentials and the model was able to predict several previously undocumented properties of the drugs.
Importance of physico‐chemical properties in determining the kinetics of the effects of Class I antiarrhythmic drugs on maximum rate of depolarization in guinea‐pig ventricle
  • T. Campbell
  • Biology, Chemistry
    British journal of pharmacology
  • 1983
TLDR
A simplified model for the interaction of Class I drugs with the fast sodium channel is proposed in which the drugs all act as ‘inactivation enhancers’ but in which their molecular weight plays a central role in determining the kinetics of this interaction.
Interval-dependent effects of small antiarrhythmic drugs on excitability of guinea-pig myocardium.
  • K. Courtney
  • Biology, Chemistry
    Journal of molecular and cellular cardiology
  • 1980
Shortening of the Action Potential and Reduction of Pacemaker Activity by Lidocaine, Quinidine, and Procainamide in Sheep Cardiac Purkinje Fibers
TLDR
The results demonstrate that lidocaine inhibits a pacemaker current which is activated on hyperpolarization and mainly carried by Na ions, and the drug inhibits a Na current, sensitive to TTX.
Antiarrhythmic agents: the modulated receptor mechanism of action of sodium and calcium channel-blocking drugs.
TLDR
This review concentrates on the antiarrhythmic drug literature pertinent to an evaluation of the modulated receptor hypothesis: lidocaine, procainamide, quinidine, diphenylhydantoin, and propranolol.
Voltage- and time-dependent depression of maximum rate of depolarisation of guinea-pig ventricular action potentials by two new antiarrhythmic drugs, flecainide and lorcainide.
TLDR
It is concluded that these long recovery times may explain the marked depression of conduction of normal sinus beats seen with these drugs.
Combined Effects of Rate, Membrane Potential, and Drugs on Maximum Rate of Rise ( Vmax) of Action Potential Upstroke of Guinea Pig Papillary Muscle
TLDR
The results help to explain the effects of an increase in rate on Vma, and conduction velocity in normal, partially depolarized, and drug-treated fibers.
...
...