Inhibitory effects of terfenadine on the rising phase of action potentials and sinus rates in isolated guinea-pig myocardium.

Inhibitory effects of terfenadine on the rising phase of action potentials and sinus rates in isolated guinea-pig myocardium.
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特非那定对离体豚鼠心肌动作电位上升期和窦性率的抑制作用。

DOI:
10.1016/0306-3623(95)02004-7
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发表时间:
1996
期刊:
General Pharmacology
影响因子:
--
通讯作者:
K. Shigenobu
K. Shigenobu
中科院分区:
--
文献类型:
--
作者:
H. Tanaka;H. Masumiya;Y. Kato;K. Shigenobu

文献摘要

被引文献

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1. 本文研究了特非那定对离体豚鼠心肌制剂心室动作电位和窦率的影响,以阐明该药是否具有心脏抑制作用。2. 特非那定显著且浓度依赖性地降低了大鼠动作电位的最大上升率(Vmax),在2 × 10 (-5) m时,其下降幅度为对照组的60%。特非那定在10 (-6)M及更高浓度时,可依赖性地降低窦率浓度;在一些制剂中,2 × 10 (-5) M(窦性停搏)时自发心跳消失。4. 另一方面,新型抗过敏药物KW-4679 ((Z)-11-[3-(二甲氨基)丙烯]-6-11-二氢二苯[b, e]奥西平-2-醋酸盐盐)的抗过敏效力高于特非那定,但对Vmax的抑制作用较弱,但不影响窦率。5. 由此可见,抗过敏药物特非那定对离体心肌有抑制作用。抗过敏药物的心脏抑制作用似乎与它们的抗过敏效力无关。
1. Effects of terfenadine on the ventricular action potential and sinus rate of isolated guinea-pig myocardial preparations were examined to elucidate whether the drug has any cardioinhibitory effect. 2. Terfenadine significantly and concentration dependently decreased the maximum rate of rise (Vmax) of action potentials, the decrease of which was 60% of the control value at 2 x 10 (-5) M. 3. Terfenadine decreased the sinus rate concentration dependently at 10 (-6) M and higher concentrations; in some preparations, spontaneous beating was abolished at 2 x 10 (-5) M (sinus arrest). 4. On the other hand, KW-4679 ((Z)-11-[3-(dimethylamino) propylidene]-6-11-dihydrodibenz [b, e] oxepin-2-acetic acid hydrochloride), a new antiallergic drug having higher antiallergic potency than terfenadine, exerted a weaker inhibitory effect on the Vmax without affecting the sinus rate. 5. In conclusion, the antiallergic drug terfenadine has inhibitory effects on isolated myocardia. The cardioinhibitory effects of antiallergic drugs seem to be independent of their antiallergic potency.