Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca2+ channels with distinct inhibitory mechanisms
Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca2+ channels with distinct inhibitory mechanisms
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DOI：
10.1159/000094900
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发表时间：
2006-01-01
期刊：
影响因子：
3.1
通讯作者：
Ono, Katsushige
中科院分区：
文献类型：
--
作者：
Lee, Tae-Seong;Kaku, Toshihiko;Ono, Katsushige
我们使用在哺乳动物细胞中分别表达的重组T型和L型Call通道，比较了依福地平和硝苯地平、二氢吡啶类似物和米贝拉地尔的详细疗效。所有这些Call通道拮抗剂均以不同的阻断方式阻断T型Call通道电流（I-Ca（T））：硝苯地平主要以紧张性方式阻断ICa（T），米贝拉地尔主要以使用依赖性方式阻断ICa（T），依福地平主要以两种方式联合阻断ICa（T）。这些Call通道拮抗剂对伊卡（T）和L型Ca ~（2+）通道电流（I-Ca（L））的IC_（50）分别为：硝苯地平1.2 μ mol/l和0.14 nmol/l，米贝拉地尔0.87和1.4 μ mol/l，依福地平0.35 μ mol/l和1.8 nmol/l。二氢吡啶类似物Efonidipine对T-型Call通道有很高的亲和力。版权所有（c）2006 S. Karger AG，巴塞尔。
We compared detailed efficacy of efonidipine and nifedipine, dihydropyridine analogues, and mibefradil using recombinant T- and L-type Call channels expressed separately in mammalian cells. All these Call channel antagonists blocked T-type Call channel currents (I-Ca(T)) with distinct blocking manners: ICa(T) was blocked mainly by a tonic manner by nifedipine, by a use-dependent manner by mibefradil, and by a combination of both manners by efonidipine. IC50S of these Call channel antagonists to ICa(T) and L-type Ca2+ channel current (I-Ca(L)) were 1.2 mu mol/l and 0.14 nmol/l for nifedipine; 0.87 and 1.4 mu mol/l for mibefradil, and 0.35 mu mol/l and 1.8 nmol/l for efonidipine, respectively. Efonidipine, a dihydropyridine analogue, showed high affinity to T-type Call channel. Copyright (c) 2006 S. Karger AG, Basel.