Use dependent depression of fast sodium current in heart muscle by the new antiarrhythmic substance Bonnecor (AWD 19-166, GS 015).
A new antiarrhythmic compound (Bonnecor AWD 19-166, GS 015) was studied in its effects on the fast sodium channel in two types of cardiac preparations (rabbit ventricular myocardium, frog atrial trabecules). AWD 19-166 depressed the maximum upstroke velocity of the action potentials in ventricular myocardium (50% inhibition at 5 X 10(-6) mol/l) and decreased the fast inward current in frog atrial myocardium. High frequent trains of pacing pulses produced a pacing dependent extra block of both the maximal upstroke velocity and the fast inward current. It is concluded that AWD 19-166 blocks the fast sodium channel in a use dependent manner.
Nilius
B
B
Benndorf
K
K
Schüttler
K
K
Boldt
W
W
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology*; D003984:Dibenzazepines / Q000494:pharmacology*; D006321:Heart / Q000187:drug effects*; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects*; D007700:Kinetics; D009206:Myocardium / Q000378:metabolism; D011817:Rabbits; D011898:Ranidae
D000889:Anti-Arrhythmia Agents; D003984:Dibenzazepines; D007473:Ion Channels; C048166:tiracizine