Influence of extracellular H+ and Ca2+ on Ro 22-9194-induced block of sodium current in cardiac myocytes

被引:0
作者
Hisatome, I [1 ]
Tanaka, Y [1 ]
Sasaki, N [1 ]
Hiroe, K [1 ]
Ahmmed, GU [1 ]
Tsuboi, M [1 ]
Manabe, I [1 ]
Suga, T [1 ]
Yamamoto, Y [1 ]
Ohtahara, A [1 ]
Kinugawa, T [1 ]
Ogino, K [1 ]
Igawa, O [1 ]
Yoshida, A [1 ]
Saito, M [1 ]
Sato, R [1 ]
Shigemasa, C [1 ]
机构
[1] NORTHWESTERN UNIV,SCH MED,DEPT MOL PHARMACOL & BIOL CHEM,CHICAGO,IL 60611
来源
GENERAL PHARMACOLOGY | 1997年 / 29卷 / 04期
关键词
Ro; 22-9194; Na+ channel; H+; Ca2+;
D O I
10.1016/S0306-3623(96)00559-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. Ro 22-9194 reduced the Na current in ventricular myocytes in either a tonic block or phasic block manner. 2. Ro 22-9194 had a higher affinity to the inactivated state (K-di=10.3 mu M) than to the rested state (K-drest=180 mu M). 3. Extracellular acidification enhanced the tonic block but reduced the phasic block. 4. Elevation of extracellular Ca2+ inhibited the enhancing effects of extracellular acidification. 5. These findings suggest that Ro 22-9194 strongly inhibits Na+ channels of the ventricular myocytes of the diseased hearts, characterized by the depolarized cell membranes and by acid conditions. (C) 1997 Elsevier Science Inc.
引用
收藏
页码:557 / 560
页数:4
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