【摘要】 本文在三种室性和一种房性心律失常的动物模型中,比较了常咯啉与奎尼丁的防治作用。又在大鼠坐骨神经上,比较了二药的局麻强度。静脉注射奎尼丁2.4—9.6mg/kg 对大鼠静脉注射乌头碱20μg/kg 引起室性心律失常的时间没有推迟作用,而常咯啉5mg/kg 能明显推迟。在大鼠静脉注射 BaCl₂ 4mg/kg 引起的室性心律失常中,静注常咯啉10mg/kg 维持正常窦性律的时间是1.8±1.6分,而静注奎尼丁4.8mg/kg 维持窦性律时间是0.2±0.6分。常咯啉抗BaCl₂心律失常的效果明显优于奎尼丁（P<0.01）。静注奎尼丁4.8mg/kg 不能提高豚鼠哇巴因中毒引起的室速和室颤阈值,仅提高室早阈值,而常略啉10mg/kg 能提高所有三个室性律阈值。在 Ach 诱发狗的房颤实验中,静注奎尼丁和常咯啉各6mg/kg 都能对抗 Ach 房颤,而且常咯啉比奎尼丁作用更强。在等毒性剂量比较下,奎尼丁是一个强的局麻药,而常咯啉则否。更多还原

【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 BaCl₂ 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.更多还原