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High throughput screening method of potassium channel regulators
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 2
- DOI:
- 10.3321/j.issn:0513-4870.2004.02.002
- Key Word:
- 钾通道阻断剂;钾通道开放剂;钙通道阻断剂;高通量筛选
Abstract： 目的建立钾通道调节剂高通量筛选的细胞模型.方法 96孔板上细胞负载荧光染料DiBAC4(3),测定不同化合物对荧光强度的影响,反映细胞膜电位的变化,间接反映化合物对钾通道的作用.结果高钾去极化和钾通道阻断剂4-AP,TEA,E-4031,glibenclamide,quinidine和nifedipine均能增强细胞的荧光强度,钾通道开放剂cromakalim能减弱细胞的荧光强度,上述化合物在一定剂量范围内均有剂量效应关系.利用该模型筛选76个化合物,发现9个化合物的荧光强度变化值有较好的剂量效应关系,有待膜片钳技术的进一步验证和筛选.结论此方法简单,易于操作,重现性好,适用于钾通道调节剂的高通量筛选.
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