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      Ro 25-6981研究進展

      發(fā)布日期:2017-11-02   瀏覽次數:1
      核心提示:a href=https://www.medchemexpress.com/ro-25-6981.htmlRo 25-6981/a產品描述:Ro 25-6981 is a potent and selective activity
      Ro 25-6981產品描述:Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM [1]Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functi


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      產品鏈接:www.medchemexpress.cn/ro-25-6981.html

       
       
       
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