Effects of amlodipine on native cardiac Na+ channels and cloned α-subunits of cardiac Na+ channels

被引：0

作者：

Inoue, Y

Hisatome, I

Tsuboi, M

Ahmmed, GU

Yatsuhashi, T

Uchida, K

Yamanouchi, Y

Santo, Y

Miake, J

Tanaka, Y

Hamada, T

Watanabe, M

Igawa, O

Yoshida, A

Shigemasa, C

Makita, N

Sato, R

机构：

[1] Tottori Univ, Fac Med, Dept Med 1, Yonago, Tottori 683, Japan

[2] Hokkaido Univ, Fac Med, Dept Med, Div Cardiol, Sapporo, Hokkaido 060, Japan

[3] Northwestern Univ, Sch Med, Dept Mol Pharmacol & Biol Chem, Chicago, IL USA

来源：

ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH | 1999年 / 49卷 / 05期

关键词：

amlodipine; effect on Na+ currents; CAS; 11470-99-6; Na+; channel; alpha-subunit; cardiac;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The inhibitory effects of amlodipine besilate (CAS 11470-99-6) on the native Na+ current (I-Na) and cloned human cardiac Na+ channel alpha subunit (hH1) were studied by whole cell patch clamp techniques. Amlodipine produced tonic block of I-Na in a concentration- and holding potential (HP)dependent manner with hyperpolarization of h(infinity). Amlodipine produced phasic blockade of I-Na, which was dependent on HP and pulse duration. Amlodipine produced tonic blockade of hH1 in a concentration-dependent manner with 1 : 1 stoichiometry, and phasic blockade of hH1 which was dependent on the pulse duration. Amlodipine blocked I-Na in a voltage- and frequency-dependent manner via affinity to the resting as well as inactivated conformations of the a subunit.

引用

页码：394 / 397

页数：4

共 12 条

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