Pharmacological investigation of a new anti-arrhythmic agent, GYKI-23 107.
GYKI-23 107 is a new antiarrhythmic substance with local anaesthetic activity. Its specific pharmacological and cardiovascular effects were studied in vivo and its efficacy was compared with that of lidocaine and mexiletine. GYKI-23 107 was effective against chemically (aconitine and ouabain) induced arrhythmias after both parenteral and oral administration. In aconitine-induced arrhythmia in mice the new compound was more active than either mexiletine or lidocaine after i.p. treatment. In ouabain-induced arrhythmia in dogs, the ED50 of GYKI-23 107 was approximately half that of mexiletine after i.v. injection. GYKI-23 107 and mexiletine produced similar elevation of the fibrillation threshold in anaesthetized cats. After oral pretreatment, GYKI-23 107 showed protective effects against coronary ligation-induced arrhythmia in conscious rats. The circulatory side-effects of GYKI-23 107 in anaesthetized and conscious dogs and cats were milder then those of mexiletine. In the antiarrhythmic dose range there were no adverse cardiovascular actions.
D031841:Aconitum; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000188:drug therapy*; D002415:Cats; D055598:Chemical Phenomena; D002621:Chemistry; D004285:Dogs; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D008012:Lidocaine / Q000627:therapeutic use; D008297:Male; D008801:Mexiletine / Q000627:therapeutic use; D051379:Mice; D010042:Ouabain; D011437:Propylamines / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats
D000889:Anti-Arrhythmia Agents; D011437:Propylamines; D008801:Mexiletine; D010042:Ouabain; C052565:GYKI 23107; D008012:Lidocaine