Development and application of Na+/Ca2+ exchange inhibitors
Development and application of Na+/Ca2+ exchange inhibitors
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DOI：
10.1023/b:mcbi.0000021367.42752.54
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发表时间：
2004-04-01
影响因子：
4.3
通讯作者：
Kita, S
中科院分区：
文献类型：
--
作者：
Iwamoto, T;Kita, S
Na+/Ca 2+交换器（NCX）是一种离子转运蛋白，根据跨质膜的离子梯度和膜电位，以Ca 2+流出或Ca 2+流入模式交换Na+和Ca 2+。在心脏、平滑肌细胞、神经元和肾单位细胞中，NCX被认为在细胞内Ca 2+浓度的调节中起重要作用。最近，一种新的选择性抑制剂（KB-R7943和SEA 0400）的Ca 2+内流模式的NCX已被开发。NCX抑制剂有望成为一种有效保护心脏和肾脏等多种器官缺血/再灌注损伤的药物。本文综述了KB-R7943和SEA 0400的药理学特性、作用的分子机制及其作为新型药物的前景。
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.