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chang ka zuo yu kui ni ding zhi liao shi yan xing xin lv shi chang de bi jiao
Pages: 23-29
Year: Issue:  1
Journal: Acta Physiologica Sinica

Keyword:  奎尼丁实验性心律失常抗心律失常药常咯啉乌头碱静脉注射哇巴因室性心律失常房颤上海药物研究所;
Abstract: Changrolin is 4-{3',5'-bis[(N-pyrrolidinyl)methyl]-4'-hydroxyanilino}quinazo-line,synthesized in our Institute.Intravenous injection of quinidine 2.4-9.6 mg/kg in anaesthetized rats couldnot delay the time of onset of arrhythmia induced by iv aconitine 20 μg/kg.Butcomplete protection from arrhythmia was seen in all the 7 rats by iv an equi-toxicdose of changrolin 5 mg/kg.In anaesthetized rats with arrhythmias induced by an iv of BaCl_2 4 mg/kg,an iv of changrolin 10 mg/kg would restore the arrhythmia to a normal sinusrhythm for 1.8±SD 1.6 minutes,which was only 0.2±0.6 min after a similariv of quinidine 4.8 mg/kg.Thus the antiarrhythmic potency of changrolin wasobviously higher than that of quinidine.Only the dose-thresholds of ouabain to induce ventricular premature beats,but not those to induce ventricular tachycardia and ventricular fibrillation,wereelevated by iv quinidine 4.8 mg/kg in anaesthetized guinea pigs.All these 3dose thresholds were,however,elevated by iv changrolin 10 mg/kg.Changrolin 6 mg/kg iv was more effective than quinidine 6 mg/kg in pro-tecting dogs from the atrial fibrillation induced by topical application of acetyl-choline.Under equitoxic doses,quinidine was a potent local anaesthetic on the sciaticnerve of rats,whilst changrolin was not.Conclusion:(1)In concordance with clinical findings,the antiarrhythmicpotency of changrolin was evidently higher than that of quinidine,while the to-xicity of changrolin was lower than that of quinidine in animals;(2)Like quinidine,changrolin effectively prevented the acetylcholine-induced auricular fibrillation.
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