Development and application of Na+/Ca2+ exchange inhibitors

被引：38

作者：

Iwamoto, T

Kita, S

机构：

[1] Fukuoka Univ, Sch Med, Dept Pharmacol, Jonan Ku, Fukuoka 8140180, Japan

[2] Natl Cardiovasc Ctr, Res Inst, Dept Mol Physiol, Osaka, Japan

来源：

MOLECULAR AND CELLULAR BIOCHEMISTRY | 2004年 / 259卷 / 1-2期

关键词：

calcium transport; inhibitor; inhibitory mechanism; ischemia/reperfusion injury; Na+/Ca2+ exchanger;

D O I：

10.1023/B:MCBI.0000021367.42752.54

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

The Na+/Ca2+ exchanger (NCX) is an ion transporter that exchanges Na+ and Ca2+ in either Ca2+ efflux or Ca2+ influx mode, depending on the ion gradients across the plasma membrane and the membrane potential. In heart, smooth muscle cells, neurons, and nephron cells, the NCX is thought to play an important role in the regulation of intracellular Ca2+ concentration. Recently, a novel selective inhibitor (KB-R7943 and SEA0400) of the Ca2+ influx mode of the NCX has been developed. NCX inhibitor is expected to be a pharmaceutical agent that offers effective protection against ischemia/reperfusion injury in several organs such as heart and kidney. Here, we summarize pharmacological profiles of KB-R7943 and SEA0400, the molecular mechanism of its action, and its future prospect as a novel pharmaceutical agent.

引用

页码：157 / 161

页数：5

共 34 条

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