L. Virag et al., Effect of GLG-V-13, a Class III antiarrhythmic agent, on potassium currents in rabbit ventricular myocytes, LIFE SCI, 66(17), 2000, pp. PL253-PL258
The effects of a new Class III antiarrhythmic drug, GLG-V-13, on the 4-amin
opyridine sensitive transient outward current, on the inward rectifier pota
ssium current, on the ATP sensitive potassium current and on the rapid and
slow components of the delayed rectifier potassium current were studied in
single rabbit ventricular myocytes using the whole-cell voltage-damp techni
que. GLG-V-13 blocked the rapid component of the delayed rectifier potassiu
m current in a dose-dependent manner, with an estimated EC50 value of 0.36
mu M. At high concentration, the slow component of the delayed rectifier po
tassium current was also depressed by the drug (40% effect at 10 mu M conce
ntration). The transient outward current, the inward rectifier potassium cu
rrent and the ATP sensitive potassium current were not influenced by GLG-V-
13, even at 10 mu M concentration. Thus, GLG-V-13 blocks predominantly the
rapid component of the delayed rectifier potassium current which may play a
significant role in the prolongation of repolarization by the drug in vent
ricular tissue. (C) 2000 Elsevier Science Inc.