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[Experimental anti-arrhythmic effects of a new beta-adrenergic receptor blocking agent, dl-l-(tert. butylamino)-3-[(2-propinyloxy)phenoxy]2-propanol hydrochloride (dl Kö 1400-Cl)].

Abstract
Antiarrhythmic property of a new adrenergic beta-blocking agent, dl-1-(tert.butylamino)-3[(2-propinyloxy) phenoxy]-2-propanol hydrochloride (Kö 1400-Cl) was studied, using 1) ouabain-induced arrhythmia in the guinea pig, 2) aconitine-induced arrhythmia in the rat, 3) arrhythmia induced by two-step ligation of coronary artery (Harris's method) in the dog and 4) halothane-adrenaline arrhythmia in the dog and was compared with those of propranolol, oxprenolol, procainamide and ajmaline. Procainamide and ajmaline produced a marked protective effect against aconitine-induced ventricular extrasystole, but were not so effective against aconitine-induced ventricular fibrillation, while oxprenolol and, to a lesser degree, propranolol were effective against the latter type of aconitine arrhythmias. Kö 1400-Cl proved to be ineffective. All the compounds tested produced a marked protective action against ouabain-arrhythmia. Whereas procainamide was most effective in abolishing the ventricular arrhythmia due to coronary-ligation even on the first postoperative day, Kö 1400-Cl and propranolol were almost ineffective on the first day. Even on the second postoperative day, the antiarrhythmic effects of these two beta-blockers were not remarkable, effective only in 2/4 animals in the case of Kö 1400-Cl and in 2/3 animals in the case of propranolol. On the contrary, all the beta-blockers tested produced a protective action against halothane-adrenaline arrhythmia at much lower doses than against coronary ligation arrhythmia. The potency ratio of Kö 1400-Cl and propranolol was 3 : 1, which paralleled with beta-blocking activity of these compounds.
AuthorsI Matsubara, K Hashimoto, Y Katano, T Tsukada, H Matsuda
JournalNihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 72 Issue 5 Pg. 557-71 (Jul 1976) ISSN: 0015-5691 [Print] JAPAN
PMID11153 (Publication Type: English Abstract, Journal Article)
Chemical References
  • Adrenergic beta-Antagonists
  • Anti-Arrhythmia Agents
  • Ouabain
  • Halothane
  • Aconitine
  • Epinephrine
Topics
  • Aconitine
  • Adrenergic beta-Antagonists (therapeutic use)
  • Animals
  • Anti-Arrhythmia Agents
  • Arrhythmias, Cardiac (chemically induced, drug therapy, etiology)
  • Dogs
  • Epinephrine
  • Female
  • Halothane
  • Ligation
  • Male
  • Ouabain
  • Rats

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