首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels
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The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels

机译:瞬时受体电位通道拮抗剂SKF96365是一种有效的低电压激活T型钙通道阻滞剂

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摘要

Background and purpose: (SKF), originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels. While SKF has been used as a tool to define the functional roles of TRPC channels in various cell and tissue types, there are notable overlapping physiological and pathophysiological associations between TRPC channels and low-voltage-activated (LVA) T-type calcium channels. The activity of SKF against T-type Ca channels has not been previously explored, and here we systematically investigated the effects of SKF on recombinant and native voltage-gated Ca channel-mediated currents.
机译:背景和目的:(SKF)最初被确定为受体介导的钙进入的阻滞剂,在诊断上被广泛使用,作为瞬时受体潜在规范型(TRPC)通道的阻滞剂。尽管SKF已被用作定义TRPC通道在各种细胞和组织类型中的功能角色的工具,但TRPC通道与低压激活(LVA)T型钙通道之间存在明显的重叠的生理和病理生理联系。 SKF对抗T型Ca通道的活性以前没有被探讨过,在这里我们系统地研究了SKF对重组和天然电压门控Ca通道介导的电流的影响。

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