Oxime depression of the fast sodium current in myocardial cells.
Effects of diacetyl monoxime on the fast Na+ current were examined by the whole-cell voltage-clamp method in embryonic chick ventricular myocytes. Diacetyl monoxime (10-20 mM) decreased the duration and amplitude of the action potential and depressed the amplitude of the peak fast inward Na+ current by about 25 (10 mM)-45% (20 mM), without affecting other I-V parameters. Neither the activation and inactivation kinetics of the Na+ channels, such as the time to peak current and the time constant of inactivation, nor the steady state characteristics of the inactivation and activation were affected by diacetyl monoxime. It also did not alter the window conductance and the recovery kinetics from inactivation (reactivation). Hence, diacetyl monoxime suppresses the fast Na+ current, without affecting the time-dependent and voltage-dependent kinetics.
Sada
H
H
Department of Pharmacology, University of Yamaguchi, College of Medicine, Ube, Japan.
Ban
T
T
Sperelakis
N
N
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D002642:Chick Embryo; D002801:Cholinesterase Reactivators / Q000494:pharmacology*; D003931:Diacetyl / Q000031:analogs & derivatives* / Q000494:pharmacology; D006329:Heart Conduction System / Q000187:drug effects; D017136:Ion Transport; D007700:Kinetics; D009206:Myocardium / Q000166:cytology*; D018408:Patch-Clamp Techniques; D012964:Sodium / Q000378:metabolism*; D015222:Sodium Channels / Q000187:drug effects* / Q000378:metabolism
D002801:Cholinesterase Reactivators; D015222:Sodium Channels; C004717:diacetylmonoxime; D012964:Sodium; D003931:Diacetyl