用于药理学筛选的基因敲除小鼠：测试钠钙交换抑制剂的特异性
Knockout mice for pharmacological screening: testing the specificity of Na+-Ca2+ exchange inhibitors.
作者信息
Reuter Hannes, Henderson Scott A, Han Tieyan, Matsuda Toshio, Baba Akemichi, Ross Robert S, Goldhaber Joshua I, Philipson Kenneth D
机构信息
Department of Physiology, David Geffen School of Medicine at UCLA, Los Angeles, Calif 90095-1760, USA.
出版信息
Circ Res. 2002 Jul 26;91(2):90-2. doi: 10.1161/01.res.0000027529.37429.38.
The role of the Na+-Ca2+ exchanger as a major determinant of cell Ca2+ is well defined in cardiac tissue, and there has been much effort to develop specific inhibitors of the exchanger. We use a novel system to test the specificity of two putative specific inhibitors, KB-R7943 and SEA0400. The drugs are applied to electrically stimulated heart tubes from control mouse embryos or embryos with the Na+-Ca2+ exchanger knocked out. We monitored effects of the drugs on Ca2+ transients. Both drugs depress the Ca2+ transients at low concentrations even in the absence of any Na+-Ca2+ exchanger. KB-R7943 and SEA0400 are not completely specific and should be used with caution as Na+-Ca2+ exchange inhibitors.
钠钙交换体作为细胞内钙离子的主要决定因素，其在心脏组织中的作用已得到明确界定，并且人们付出了很多努力来开发该交换体的特异性抑制剂。我们使用一种新型系统来测试两种假定的特异性抑制剂KB-R7943和SEA0400的特异性。将这些药物应用于来自对照小鼠胚胎或敲除了钠钙交换体的胚胎的电刺激心脏管。我们监测了药物对钙离子瞬变的影响。即使在没有任何钠钙交换体的情况下，这两种药物在低浓度时也会抑制钙离子瞬变。KB-R7943和SEA0400并非完全特异性，作为钠钙交换抑制剂使用时应谨慎。
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