KB-R7943抑制培养的神经元和星形胶质细胞中的钙库操纵性钙内流。
KB-R7943 inhibits store-operated Ca(2+) entry in cultured neurons and astrocytes.
作者信息
Arakawa N, Sakaue M, Yokoyama I, Hashimoto H, Koyama Y, Baba A, Matsuda T
机构信息
Laboratory of Neuropharmacology, Laboratory of Medicinal Pharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka, 565-0871, Japan.
出版信息
Biochem Biophys Res Commun. 2000 Dec 20;279(2):354-7. doi: 10.1006/bbrc.2000.3968.
We have studied cyclopiazonic acid (CPA)-sensitive store-operated Ca(2+) entry (SOCE) in cultured neurons and astrocytes and examined the effect of 2-[2-[4-(4-nitrobenzyloxy)phenyl]]isothiourea (KB-R7943), which is often used as a selective inhibitor of the Na(+)-Ca(2+) exchanger (NCX), on the SOCE. CPA increased transiently intracellular Ca(2+) concentration (Ca(2+)) followed by a sustained increase in Ca(2+) in neurons and astrocytes. The sustained increase in Ca(2+) depended on the presence of extracellular Ca(2+) and inhibited by SOCE inhibitors, but not by a Ca(2+) channel inhibitor. CPA also caused quenching of fura-2 fluorescence when the cells were incubated in Mn(2+)-containing medium. KB-R7943 at 10 microM inhibited significantly CPA-induced sustained increase in Ca(2+) in neurons and astrocytes. KB-R7943 also inhibited CPA-induced quenching of fura-2 fluorescence in the presence of extracellular Mn(2+). These results indicate that cultured neurons and astrocytes possess SOCE and that KB-R7943 inhibits not only NCX but also SOCE.
我们研究了培养的神经元和星形胶质细胞中对环匹阿尼酸（CPA）敏感的储存式钙（Ca²⁺）内流（SOCE），并检测了常被用作钠钙交换体（NCX）选择性抑制剂的2-[2-[4-(4-硝基苄氧基)苯基]]异硫脲（KB-R7943）对SOCE的影响。CPA使神经元和星形胶质细胞内的细胞内钙浓度（[Ca²⁺]i）短暂升高，随后[Ca²⁺]i持续升高。[Ca²⁺]i的持续升高依赖于细胞外钙的存在，并被SOCE抑制剂抑制，但不被钙通道抑制剂抑制。当细胞在含锰（Mn²⁺）的培养基中孵育时，CPA还会导致fura-2荧光淬灭。10微摩尔的KB-R7943显著抑制了CPA诱导的神经元和星形胶质细胞中[Ca²⁺]i的持续升高。在细胞外存在Mn²⁺的情况下，KB-R7943也抑制了CPA诱导的fura-2荧光淬灭。这些结果表明，培养的神经元和星形胶质细胞具有SOCE，并且KB-R7943不仅抑制NCX，还抑制SOCE。
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