Glimepiride块克隆β细胞,心肌和平滑肌K (ATP)通道。

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歌DK,阿什克罗夫特调频

Glimepiride块克隆β细胞,心肌和平滑肌K (ATP)通道。

Br杂志。2001;133 (1):193 - 9。

PubMed ID

11325810 (在PubMed

]

文摘

1。我们检查的效果磺脲glimepiride在三种类型的重组ATP-sensitive钾(K (ATP)通道。2。K (ATP)通道共享一个共同的成孔单元,Kir6.2,同事磺脲受体不同亚型(SUR1细胞,在心脏和SUR2B SUR2A平滑肌)。3所示。Kir6.2与SUR1 coexpressed, SUR2A或SUR2B非洲爪蟾蜍卵母细胞和宏观K (ATP)电流记录从巨大的由内向外膜补丁。Glimepiride被加入到细胞内的膜表面。4所示。Glimepiride抑制Kir6.2 /苏尔电流与两个网站:一个低亲和力网站Kir6.2 (IC(50) =大约400 microM)和高亲和性位点与苏尔(SUR1 IC (50) = 3.0 nM, 5.4 nM SUR2A SUR2B和7.3 nM)。的效力glimepiride高亲和性网站接近观察的格列本脲(SUR1 4海里,27 nM SUR2A),也有类似的结构。 5. Glimepiride inhibition of Kir6.2/SUR2A and Kir6.2/SUR2B currents, but not Kir6.2/SUR1 currents, reversed rapidly. 6. Our results indicate that glimepiride is a high-affinity sulphonylurea that does not select between the beta-cell, cardiac and smooth muscle types of recombinant K(ATP) channel, when measured in inside-out patches. High-affinity inhibition is mediated by interaction of the drug with the sulphonylurea receptor subunit of the channel.

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药物靶点

药物	目标	类	生物	药理作用	行动
Glimepiride	ATP-sensitive内向整流钾通道11	蛋白质	人类	是的	抑制剂	细节