四丙酰关附醇胺的抗心律失常作用及其与关附甲素的比较

在几种动物模型上观察了四丙酰关附醇胺(TPGFA)的抗心律失常作用. TPGFA使引发室性早搏，室性心动过速和心室纤颤所需乌头碱用量增加50%的剂量分别为1.6，1.4和1.8 mg·kg^-1；TPGFA 2 mg·kg^-1可提高豚鼠心脏毒毛花苷G中毒的耐受量和家兔心脏电致室颤阈；TPGFA还降低CaCl₂诱发的大鼠室颤发生率和死亡率，以及麻醉大鼠心脏冠脉结扎—再灌性室性心动过速和室颤的发生率. TPGFA的上述抗心律失常作用较关附甲素强. TPGFA显著延长大鼠心电图的QT_c间期，而对P-R间期和QRS时程影响不明显. 小鼠iv TPGFA的LD₅₀为42 mg·kg^-1.

Antiarrhythmic effects of tetrapropinyl guan-fu alcohol amine and the comparison with guan-fu base A1

The antiarrhythmic effects of tetrapropinyl guan-fu alcohol amine (TPGFA) in several animal models were investigated. TPGFA 1, 2 and 4 mg·kg^-1 iv significantly counteracted arrhythmia induced by aconitine in rats, and increased the doses of strophantin G to produce ventricular premature beats (VP), ventricular tachycardia (VT), ventricular fibrillation (VF) and cardiac arrest (CA) in guinea pigs. Pretreatment of rats with TPGFA 7 and 10 mg·kg^-1 iv significantly reduced the incidence of VF induced by CaCl₂ and reduced the mortality as well. The ventricular fibrillation threshold for electrical stimulation was elevated by TPGFA 2, 4 and 8 mg·kg^-1 iv in rabbits. VT and VF due to the coronary artery ligation and reperfusion could be prevented by TPGFA (4.5, 6 and 8 mg·kg^-1 iv) in anesthetized rats. The antiarrhythmic effects of TPGFA were more potent than those of guan-fu base A. TPGFA did not alter the P-R interval or QRS duration but increased the QT_c interval significantly in electrocardiogram. The LD₅₀ of TPGFA in mice was 42 mg·kg^-1 iv.