ATP-sensitive钾通道的抑制小鼠胰岛细胞表面活性剂。

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史密斯PA, Proks P

ATP-sensitive钾通道的抑制小鼠胰岛细胞表面活性剂。

Br J杂志。1998年6月,124 (3):529 - 39。

PubMed ID

9647478 (在PubMed

]

文摘

1。我们使用膜片钳方法研究的影响洗涤剂,Cremophor,二层80和特里同X100 K (ATP)通道在小鼠的胰腺β细胞。2。所有三个洗涤剂阻塞K (ATP)通道活动与以下的效力顺序:渐变80 (Ki <大约83海里)> Triton X100 > Cremophor (Ki = 350海里)。在所有情况下,块是不可逆的。3所示。单通道的研究表明,在低剂量的洗涤剂作为慢阻滞剂K (ATP)通道。4所示。不同于块由甲苯磺丁脲,由洗涤剂不受细胞内Mg2 +核苷酸,氯甲苯噻嗪或胰岛素治疗,也没有涉及一个加速度的纲要或增加ATP敏感性的香奈儿。5。 The detergents could block the pore-forming subunit, Kir6.2deltaC26, which can be expressed independently of SUR1 (the regulatory subunit of the K(ATP) channel). These data suggest that the detergents act on Kir6.2 and not SUR1. 6. The detergents had no effect on another member of the inward rectifier family: Kir1.1a (ROMK1). 7. Voltage-dependent K-currents in the beta-cell were reversibly blocked by the detergents with a far lower potency than that found for the K(ATP) channel. 8. Like other insulin secretagogues that act by blocking the K(ATP) channel, Cremophor elevated intracellular Ca2+ in single beta-cells to levels that would be expected to elicit insulin secretion. 9. Given the role of the K(ATP) channel in many physiological processes, we conclude that plasma borne detergent may have pharmacological actions mediated through blockage of the K(ATP) channel.

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药物靶点

药物	目标	类	生物	药理作用	行动
甲苯磺丁脲	ATP-sensitive内向整流钾通道1	蛋白质	人类	未知的	抑制剂	细节