4-{3′,5′-双-[(N-吡咯烷基)甲基]-4′-羟苯胺基}喹唑啉(常咯啉)抗乌头硷诱发大鼠心律失常的作用

大鼠静注常咯啉再注射乌头硷,或同时用常咯啉和乌头硷,明显推迟乌头硷引起的心律紊乱。先静注乌头硷出现心律失常后,再注射常咯啉,抗心律失常作用较弱。剪断二侧迷走神经,或静注六烃季铵,都不影响常咯啉抗静注乌头硷所致心律失常的疗效。从静脉恒速注射乌头硷,记录室性早搏、室性心动过速和心室颤动阈值。预先静脉注射常咯啉明显提高这三种阈值。利血平化加常咯啉组,这些阀值也比对照组明显提高,与常咯啉组相比,仅显著提高心室颤动阈值。脑室内注射常咯啉后,再脑室内注射乌头硷,明显推迟心律失常出现时间。常咯啉对大鼠坐骨神经的局麻作用甚微,这与利多卡因有明显不同。

ANTIARRHYTHMIC EFFECT OF 4-{3', 5'-BIS [(N-PYRRO LIDINYL)METHYL]-4'-HYDROXYANILINO} QUINAZOLINE (CHANGROLIN) ON ACONITINE-INDUCED ARRHYTHMIA IN RATS

Intravenous injections of changrolin followed by or concomitant with injections of aconitine could retard the onset of aconitineinduced arrhythmia. If changrolin was given after the onset of arrhythmia, the antiarrhythmic effect of changrolin would be weaker. Neither bilateral vagotomy nor intravenous injections of hexamethonium modified the antiarrhythmic effect of changrolin. The dose thresholds for ventricular premature beats, ventricular tachycardia and ventricular fibrillation during intravenous infusion of aconitine at constant rate were all raised by a premedication of changrolin, and further augmented by a previous reserpinization. Administrations of changrolin into the lateral cerebral ventricle also retarded the onset of arrhythmia induced by a subsequent intracerebral introduction of aconitine.On the sciatic nerves of rats changrolin manifestated only a very mild local anaesthetic action, which was obviously different from that of lidocaine.