阿普林定和奎尼丁对豚鼠心肌Vmax阻滞作用的比较研究。
Comparative study of the block of Vmax by aprindine and quinidine in the guinea-pig heart muscle.
作者信息
Hisatome I, Miyamoto J, Hasegawa J, Kotake H, Mashiba H, Sato R
机构信息
1st Department of Internal Medicine, Tottori University School of Medicine, Yonago, Japan.
出版信息
Eur J Pharmacol. 1988 Aug 24;153(2-3):285-8. doi: 10.1016/0014-2999(88)90616-4.
The depression of Vmax of the action potential in guinea-pig ventricular muscle by aprindine and quanidine was compared. Aprindine caused a more pronounced rate-dependent block (Kd = 10(-6) M at 3.3 Hz) than did quinidine (Kd = 1.6 X 10(-5) M at 3.3 Hz). Aprindine shifted the relationship between Vmax and resting potential to a more negative potential (mean 9.2 mV: 10 microM) than did quinidine (mean 5.7 mV: 10 microM). In addition, aprindine caused a more pronounced resting block (Kd = 1.3 X 10(-5) M) than quinidine (Kd = 8.6 X 10(-5) M). It is concluded that aprindine has a higher affinity for activated and/or inactivated and resting state channels than quinidine, making channels unavailable for conduction upon activation.
比较了阿普林定和奎尼丁对豚鼠心室肌动作电位Vmax的抑制作用。与奎尼丁（在3.3Hz时Kd = 1.6×10⁻⁵M）相比，阿普林定引起更明显的频率依赖性阻滞（在3.3Hz时Kd = 10⁻⁶M）。与奎尼丁（10μM时平均为5.7mV）相比，阿普林定使Vmax与静息电位之间的关系向更负的电位偏移（10μM时平均为9.2mV）。此外，与奎尼丁（Kd = 8.6×10⁻⁵M）相比，阿普林定引起更明显的静息阻滞（Kd = 1.3×10⁻⁵M）。结论是，与奎尼丁相比，阿普林定对激活和/或失活及静息状态通道具有更高的亲和力，使得通道在激活时无法用于传导。
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