High affinity binding of a potassium channel agonist to intact rat insulinoma cells.
High affinity binding of a potassium channel agonist to intact rat insulinoma cells.
复制标题
钾通道激动剂与完整大鼠胰岛素瘤细胞的高亲和力结合。
DOI：
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发表时间：
1993
期刊：
影响因子：
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通讯作者：
R. Janis
中科院分区：
文献类型：
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作者：
F. Hoffman;J. Lenfers;E. Niemers;U. Pleiss;A. Scriabine;R. Janis
一种新型的氚化钾通道开放剂[~3H] BAY X 9228在大鼠胰岛素瘤（RINm5F）细胞系中的特异性结合已被表征。通过饱和分析测定，KD为2.1 nM，Bmax为50 fmol/mg总蛋白。与完整细胞的高亲和力结合被吡那地尔和一系列BAY X 9228类似物抑制，所述BAY X 9228类似物具有与产生部分去极化大鼠主动脉的格列本脲可逆松弛的活性序列相关的活性序列。这代表了K+通道开放剂与培养细胞特异性结合的首次报道。
The specific binding of a novel tritiated K+ channel opener, [3H]BAY X 9228, has been characterized in a rat insulinoma (RINm5F) cell line. The KD was 2.1 nM and Bmax 50 fmol/mg total protein as determined by saturation analysis. The high affinity binding to intact cells was inhibited by pinacidil and by a series of BAY X 9228 analogs with an activity sequence correlating well with that for producing glyburide-reversible relaxation of partially depolarized rat aorta. This represents the first report of the specific binding of a K+ channel opener to cultured cells.